- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- 新產品
- 聯(lián)系我們
別名: ZD1839 中文名稱:吉非替尼
Gefitinib是一種EGFR抑制劑,作用于NR6wtEGFR和NR6W細胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分別為37 nM、37nM、26 nM和57 nM。Gefitinib 可通過阻滯PI3K/AKT/mTOR信號通路來促進肺癌細胞的自噬和細胞凋亡。
Gefitinib Chemical Structure
CAS: 184475-35-2
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
---|---|---|---|---|---|
MIAPaCa2 | Apoptosis Assay | 20 μM | 24 h | does not induce apoptosis assessed as caspase 3 activation | 20466555 |
MIAPaCa2 | Apoptosis Assay | 10 μM | 24h or 48 h | does not induce apoptosis | 20466555 |
MIAPaCa2 | Cytotoxic Assay | 1 μM | 10 d | has no cytotoxicity assessed as suppression of colony formation | 20466555 |
MIAPaCa2 | Growth Inhibition Assay | 2.5 μM | 72 h | has no growth inhibition | 20466555 |
H1975 | Kinase Assay | 0.5 μM | 24 h | does not inhibit EGFR L858R/T790M mutant-mediated Akt phosphorylation | 22339342 |
H1975 | Kinase Assay | 0.5 μM | 24 h | does not inhibit EGFR L858R/T790M mutant-mediated Erk phosphorylation | 22339342 |
H1975 | Kinase Assay | 0.125 μM | 24 h | does not inhibit EGFR L858R/T790M mutant Y1068 autophosphorylation | 22339342 |
H1975 | Kinase Assay | 0.33 μM | 2 h | does not inhibit EGFR L858R/T790M double mutant phosphorylation | 24124898 |
H1975 | Kinase Assay | 0.33 μM | 2 h | does not inhibit EGFR L858R/T790M double mutant assessed as reduction in ERK phosphorylation | 24124898 |
H1975 | Kinase Assay | 0.33 μM | 2 h | does not inhibit EGFR L858R/T790M double mutant assessed as reduction in AKT phosphorylation | 24124898 |
HCC827 | Kinase Assay | 0.11 μM | 1 h | has no irreversible inhibition of EGFR assessed as recovery of EGFR autophosphorylation | 24124898 |
H1975 | Function Assay | 1 μM | 24 h | does not inhibit ERK phosphorylation in human H1975 cells harboring EGFR L858R/T790M | 24607591 |
H1975 | Kinase Assay | 1 μM | 24 h | does not inhibit EGFR phosphorylation in human H1975 cells harboring EGFR L858R/T790M mutant | 24607591 |
LNCaP | Function Assay | 10 μM | 2h or 4 h | does not inhibit autophosphorylation of immunopurified flag-tagged Bmx assessed as incorporation of [32P]ATP | 18667312 |
A431 | Kinase Assay | 1 μM | 1 h | has no irreversible inhibition of EGFR autophosphorylation | 24900594 |
NCI-H1975 | Function Assay | 10 μM | 8 h | does not inhibiti EGFR assessed as reduction in ERK phosphorylation | 23116168 |
HCC827 | Cytotoxic Assay | 0.5 μM | 72 h | has no cytotoxicity | 23993328 |
HCC827 | Function Assay | 0.5 μM | 2 h | does not inhibit c-Met assessed as inhibition of p44/42 phosphorylation | 23993328 |
HCC827 | Function Assay | 0.5 μM | 2 h | does not inhibit c-Met assessed as inhibition of AKT phosphorylation | 23993328 |
NCI-H1975 | Function Assay | 100 μM | 150 min | Induction of NO production in human NCI-H1975 cells harboring EGFR L858R/T790M mutant | 24607591 |
BEAS2B | Growth Inhibition Assay | 50 μM | 72 h | IC50=13.94 μM | 24607591 |
KB | Kinase Assay | 10 μM | 1 h | Inhibition of EGF-stimulated autophosphorylation of EGFR with IC50 of 0.025 μM | 24411123 |
MDCK2 | Function Assay | 1.8 μM | 72 h | Inhibition of human BCRP expressed assessed as Hoechst 33342 accumulation with IC50 of 3.19 μM | 24184213 |
BCRP-MDCK2 | Function Assay | 1.8 μM | 72 h | Reduction of plasma membrane expression of BCRP expressing reporter gene GFP | 24184213 |
BCRP-MDCK2 | Function Assay | 1.8 μM | 72 h | Increase of plasma membrane expression of BCRP expressing reporter gene GFP | 24184213 |
A431 | Kinase Assay | 100 μM | 30 min | Inhibition of EGFR in shed membrane vesicles with IC50 of 1.1 μM | 24094432 |
HCC827 | Growth Inhibition Assay | 10 μM | 72 h | Antiproliferative activity against gefitinib-sensitive human HCC827 cells harboring EGFR E746 to A750 deletion with IC50 of 0.00581 μM | 24053674 |
HCC827 | Function Assay | 0.5 μM | 2 h | Inhibition of c-Met phosphorylation in gefitinib-resistant human HCC827 cells | 23993328 |
HCC827 | Kinase Assay | 0.5 μM | 2 h | Inhibition of EGFR phosphorylation in gefitinib-resistant human HCC827 cells | 23993328 |
A549 | Function Assay | 1 μM | 1 h | Cellular uptake | 23988354 |
A549 | Kinase Assay | 1 μM | 1 h | Inhibition of EGFR autophosphorylation with IC50 of 0.0399 μM | 23988354 |
16HBE | Function Assay | 100 μM | 150 min | Induction of nitric oxide production in human 16HBE cells expressing wild type EGFR | 23792318 |
NCI-H1975 | Cytotoxic Assay | 10 μM | 72 h | Cytotoxicity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition with IC50 of 6.917 μM | 23668441 |
16HBE14o- | Cytotoxic Assay | 10 μM | 72 h | Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition with IC50 of 12.71 μM | 23668441 |
PC9 | Growth Inhibition Assay | 10 μg/mL | 72 h | IC50=0.014 μM | 23116168 |
HCC827 | Cytotoxic Assay | 10 μg/mL | 72 h | IC50=0.0015 μM | 23116168 |
FADU | Cytotoxic Assay | 10 μg/mL | 72 h | IC50=0.05 μM | 23116168 |
Calu3 | Cytotoxic Assay | 10 μg/mL | 72 h | IC50=1.6 μM | 23116168 |
A431 | Kinase Assay | 100 μM | 30 min | Inhibition of EGFR derived from human A431 cell membrane assessed as inhibition of poly-Glu-Tyr phosphorylation with IC50 of 1.08 μM | 22698782 |
HCC827 | Kinase Assay | 0.125 μM | 24 h | Inhibition of EGFR del E746-A750 mutant-mediated Akt phosphorylation | 22339342 |
HCC827 | Kinase Assay | 0.125 μM | 24 h | Inhibition of EGFR del E746-A750 mutant-mediated Erk phosphorylation | 22339342 |
HCC827 | Kinase Assay | 0.125 μM | 24 h | Inhibition of EGFR del E746-A750 mutant Y1068 autophosphorylation | 22339342 |
MCF7 | Cytotoxic Assay | 10 μM | 48 h | Cytotoxicity against serum-starved human MCF7 cells over-expressing ErbB2 cells | 22138308 |
BT474 | Cytotoxic Assay | 10 μM | 48 h | Cytotoxicity against serum-starved human BT474 cells | 22138308 |
MCF7 | Growth Inhibition Assay | 100?μg/mL | 48 h | Antiproliferative activity against human MCF7 cells overexpressing EGFR gene with IC50 of 12.05 μM | 22119130 |
MDA-MB-468 | Growth Inhibition Assay | 100 μM | 48 h | Antiproliferative activity | 21429632 |
PC3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=7.4 μM | 21353546 |
NCI-H1975 | Function Assay | 5 μM | 48 h | Induction of apoptosis assessed as activation of caspase-3 | 20151670 |
NCI-H1975 | Growth Inhibition Assay | 5 μM | 72 h | IC50=8.26 μM | 20151670 |
A431 | Kinase Assay | 100 μM | 10 min | Prolonged inhibitory activity of EGF-induced EGFR phosphorylation | 19969465 |
A431 | Kinase Assay | 0.1 μM | 1 h | Inhibition of EGF-induced EGFR phosphorylation | 19969465 |
A431 | Growth Inhibition Assay | 10 μM | 72 h | GI50=0.514 μM | 19969465 |
MCF7 | Cytotoxic Assay | 50 μM | 72 h | IC50=12.05 μM | 18771819 |
NIH3T3 | Function Assay | 0.2 μM | 2 h | Inhibition of EGF stimulated human erbB1 autophosphorylation with IC50 of 0.0144 μM | 16480284 |
NCI-H1975 | Function Assay | 10 μM | Inhibition of ERBB2 autophosphorylation | 20151670 | |
NCI-H1975 | Kinase Assay | 10 μM | Inhibition of EGFR autophosphorylation | 20151670 | |
COS7 | Function Assay | 96 μM | Inhibition of human JAK2 V617F mutant expressed | 17178722 | |
SW620 | Cytotoxic Assay | 48 h | IC50=28.2 μM | 24900594 | |
Sf9 | Kinase Assay | 10 min | Inhibition of autophosphorylation of recombinant his-tagged EGFR (amino acid 645-1186) expressed with IC50 of 0.02 μM | 24731281 | |
HepG2 | Growth Inhibition Assay | 24 h | IC50=6.42 μM | 24731281 | |
Hela | Growth Inhibition Assay | 24 h | IC50=2.67 μM | 24731281 | |
Calu3 | Cytotoxic Assay | 72 h | Cytotoxicity against human Calu3 cells expressing HER2 with IC50 of 0.99 μM | 24411123 | |
A431 | Cytotoxic Assay | 72 h | Cytotoxicity against human A431 cells expressing EGFR with IC50 of 0.55 μM | 24411123 | |
MDCK | Cytotoxic Assay | 72 h | GI50=1.45 μM | 24184213 | |
HCC827 | Growth Inhibition Assay | 72 h | IC50=0.012 μM | 23973168 | |
PC9 | Kinase Assay | 2 h | Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells with IC50 of 0.0087 μM | 23930994 | |
LoVo | Kinase Assay | 2 h | Inhibition of EGFR phosphorylation with IC50 of 0.062 μM | 23930994 | |
SH-SY5Y | Cytotoxic Assay | 72 h | IC50=18.21 μM | 23871909 | |
A549 | Growth Inhibition Assay | 72 h | Antiproliferative activity against wild type EGFR/k-Ras dependent human A549 cells with IC50 of 4.626 μM | 23792318 | |
16HBE | Growth Inhibition Assay | 72 h | Antiproliferative activity against human 16HBE cells expressing wild type EGFR with IC50 of 1.601 μM | 23792318 | |
Sf9 | Kinase Assay | 1 h | Inhibition of human GST-tagged EGFR L834R mutant expressed with IC50 of 0.015 μM | 23611691 | |
SGC7901 | Cytotoxic Assay | 72 h | IC50=10.26 μM | 22727449 | |
HT-29 | Cytotoxic Assay | 72 h | IC50=3.36 μM | 22727449 | |
H460 | Cytotoxic Assay | 72 h | IC50=5.59 μM | 22727449 | |
A431 | Kinase Assay | 2 h | Inhibition of EGFR phosphorylation in EGF-stimulated human A431 with IC50 of 0.001 μM | 22101132 | |
NCI-H292 | Growth Inhibition Assay | 72 h | IC50=0.02 μM | 21916433 | |
NCI-H1993 | Growth Inhibition Assay | 72 h | IC50=0.1 μM | 21916433 | |
PANC1 | Cytotoxic Assay | 5 d | IC50=40.42 μM | 20466555 | |
MIAPaCa2 | Cytotoxic Assay | 5 d | IC50=50.62 μM | 20466555 | |
DU145 | Cytotoxic Assay | 5 d | IC50=42.17 μM | 20466555 | |
SMMC7721 | Growth Inhibition Assay | 48 h | IC50=33.12 μM | 20304537 | |
A375 | Growth Inhibition Assay | 48 h | IC50=20.55 μM | 20304537 | |
Sf9 | Kinase Assay | 10 min | Inhibition of EGFR expressed assessed as inhibition of receptor autophosphorylation with IC50 of 0.033 μM | 20056425 | |
MCF7 MX | Function Assay | 30 min | Inhibition of BCRP expressed with IC50 of 1.1 μM | 19932960 | |
NIH3T3 | Growth Inhibition Assay | 72 h | Growth inhibition of mouse NIH/3T3 cells expressing erB2 gene with IC50 of 0.54 μM | 19665377 | |
BA/F3 | Cytotoxic Assay | 72 h | Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant with IC50 of 0.0108 μM | 19239229 | |
HN5 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human HN5 cells overexpressing EGFR with EC50 of 0.01 μM | 19028424 | |
BT474 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human BT474 cells overexpressing ERBb2 with EC50 of 0.3 μM | 19028424 | |
MOLT4 | Cytotoxic Assay | 96 h | IC50=15.02 μM | 18313807 | |
MDA-MB-231 | Cytotoxic Assay | 96 h | IC50=36.61 μM | 18313807 | |
K562 | Cytotoxic Assay | 96 h | IC50=9.36 μM | 18313807 | |
A549 | Cytotoxic Assay | 96 h | IC50=13.59 μM | 18313807 | |
NCI-H209 | Growth Inhibition Assay | IC50=1.77269 μM | SANGER | ||
EPLC-272H | Growth Inhibition Assay | IC50=1.85549 μM | SANGER | ||
OMC-1 | Growth Inhibition Assay | IC50=1.99888 μM | SANGER | ||
HCC70 | Growth Inhibition Assay | IC50=2.00815 μM | SANGER | ||
CAL-12T | Growth Inhibition Assay | IC50=2.01861 μM | SANGER | ||
TGBC24TKB | Growth Inhibition Assay | IC50=2.02961 μM | SANGER | ||
EKVX | Growth Inhibition Assay | IC50=2.04939 μM | SANGER | ||
SW1116 | Growth Inhibition Assay | IC50=2.06009 μM | SANGER | ||
NCI-H2009 | Growth Inhibition Assay | IC50=2.06214 μM | SANGER | ||
RPMI-8866 | Growth Inhibition Assay | IC50=2.08481 μM | SANGER | ||
KARPAS-45 | Growth Inhibition Assay | IC50=2.12479 μM | SANGER | ||
RXF393 | Growth Inhibition Assay | IC50=2.13036 μM | SANGER | ||
786-0 | Growth Inhibition Assay | IC50=2.18406 μM | SANGER | ||
SCC-4 | Growth Inhibition Assay | IC50=2.21776 μM | SANGER | ||
BT-20 | Growth Inhibition Assay | IC50=2.26744 μM | SANGER | ||
A498 | Growth Inhibition Assay | IC50=2.29415 μM | SANGER | ||
IGROV-1 | Growth Inhibition Assay | IC50=2.31237 μM | SANGER | ||
JVM-3 | Growth Inhibition Assay | IC50=2.34643 μM | SANGER | ||
NCI-H2170 | Growth Inhibition Assay | IC50=2.34783 μM | SANGER | ||
EW-18 | Growth Inhibition Assay | IC50=2.35471 μM | SANGER | ||
KU812 | Growth Inhibition Assay | IC50=2.36779 μM | SANGER | ||
NY | Growth Inhibition Assay | IC50=2.3727 μM | SANGER | ||
HTC-C3 | Growth Inhibition Assay | IC50=2.42267 μM | SANGER | ||
CFPAC-1 | Growth Inhibition Assay | IC50=2.43864 μM | SANGER | ||
HH | Growth Inhibition Assay | IC50=2.49854 μM | SANGER | ||
MKN7 | Growth Inhibition Assay | IC50=2.62748 μM | SANGER | ||
TE-8 | Growth Inhibition Assay | IC50=2.63653 μM | SANGER | ||
MC-IXC | Growth Inhibition Assay | IC50=2.64453 μM | SANGER | ||
DMS-79 | Growth Inhibition Assay | IC50=2.69284 μM | SANGER | ||
Detroit562 | Growth Inhibition Assay | IC50=2.69845 μM | SANGER | ||
HuP-T4 | Growth Inhibition Assay | IC50=2.72818 μM | SANGER | ||
QIMR-WIL | Growth Inhibition Assay | IC50=2.75952 μM | SANGER | ||
BB65-RCC | Growth Inhibition Assay | IC50=2.80713 μM | SANGER | ||
PC-3 | Growth Inhibition Assay | IC50=2.83317 μM | SANGER | ||
OVCAR-3 | Growth Inhibition Assay | IC50=2.85594 μM | SANGER | ||
KYSE-510 | Growth Inhibition Assay | IC50=2.86786 μM | SANGER | ||
HC-1 | Growth Inhibition Assay | IC50=2.94012 μM | SANGER | ||
NCI-H1693 | Growth Inhibition Assay | IC50=2.95897 μM | SANGER | ||
DU-4475 | Growth Inhibition Assay | IC50=2.99052 μM | SANGER | ||
COLO-680N | Growth Inhibition Assay | IC50=3.00495 μM | SANGER | ||
MN-60 | Growth Inhibition Assay | IC50=3.04974 μM | SANGER | ||
BCPAP | Growth Inhibition Assay | IC50=3.08295 μM | SANGER | ||
647-V | Growth Inhibition Assay | IC50=3.1622 μM | SANGER | ||
HT-1376 | Growth Inhibition Assay | IC50=3.20506 μM | SANGER | ||
NCI-H1793 | Growth Inhibition Assay | IC50=3.21098 μM | SANGER | ||
SW1463 | Growth Inhibition Assay | IC50=3.26192 μM | SANGER | ||
NCI-H727 | Growth Inhibition Assay | IC50=3.38584 μM | SANGER | ||
LB771-HNC | Growth Inhibition Assay | IC50=3.39126 μM | SANGER | ||
D-542MG | Growth Inhibition Assay | IC50=3.44222 μM | SANGER | ||
NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=3.44957 μM | SANGER | ||
C8166 | Growth Inhibition Assay | IC50=3.46521 μM | SANGER | ||
639-V | Growth Inhibition Assay | IC50=3.57792 μM | SANGER | ||
TE-1 | Growth Inhibition Assay | IC50=3.59169 μM | SANGER | ||
OAW-28 | Growth Inhibition Assay | IC50=3.59426 μM | SANGER | ||
SK-LU-1 | Growth Inhibition Assay | IC50=3.60645 μM | SANGER | ||
CaR-1 | Growth Inhibition Assay | IC50=3.61048 μM | SANGER | ||
A2780 | Growth Inhibition Assay | IC50=3.64089 μM | SANGER | ||
C2BBe1 | Growth Inhibition Assay | IC50=3.64407 μM | SANGER | ||
SK-MES-1 | Growth Inhibition Assay | IC50=3.64614 μM | SANGER | ||
PANC-10-05 | Growth Inhibition Assay | IC50=3.72072 μM | SANGER | ||
J-RT3-T3-5 | Growth Inhibition Assay | IC50=3.75406 μM | SANGER | ||
ES4 | Growth Inhibition Assay | IC50=3.82286 μM | SANGER | ||
NCI-H28 | Growth Inhibition Assay | IC50=3.82961 μM | SANGER | ||
NCI-H1155 | Growth Inhibition Assay | IC50=3.84159 μM | SANGER | ||
KURAMOCHI | Growth Inhibition Assay | IC50=3.86056 μM | SANGER | ||
NCI-H69 | Growth Inhibition Assay | IC50=3.90178 μM | SANGER | ||
IST-MES1 | Growth Inhibition Assay | IC50=3.94029 μM | SANGER | ||
NH-12 | Growth Inhibition Assay | IC50=3.94187 μM | SANGER | ||
JVM-2 | Growth Inhibition Assay | IC50=3.94752 μM | SANGER | ||
EW-16 | Growth Inhibition Assay | IC50=3.95577 μM | SANGER | ||
NCI-H441 | Growth Inhibition Assay | IC50=3.97014 μM | SANGER | ||
RCC10RGB | Growth Inhibition Assay | IC50=4.01246 μM | SANGER | ||
TCCSUP | Growth Inhibition Assay | IC50=4.1105 μM | SANGER | ||
HL-60 | Growth Inhibition Assay | IC50=4.12241 μM | SANGER | ||
EW-11 | Growth Inhibition Assay | IC50=4.13261 μM | SANGER | ||
KARPAS-299 | Growth Inhibition Assay | IC50=4.31013 μM | SANGER | ||
SNU-C2B | Growth Inhibition Assay | IC50=4.34686 μM | SANGER | ||
LU-139 | Growth Inhibition Assay | IC50=4.37247 μM | SANGER | ||
HCC1937 | Growth Inhibition Assay | IC50=4.37993 μM | SANGER | ||
GR-ST | Growth Inhibition Assay | IC50=4.4318 μM | SANGER | ||
SK-OV-3 | Growth Inhibition Assay | IC50=4.46042 μM | SANGER | ||
A172 | Growth Inhibition Assay | IC50=4.55521 μM | SANGER | ||
NB10 | Growth Inhibition Assay | IC50=4.59781 μM | SANGER | ||
P30-OHK | Growth Inhibition Assay | IC50=4.81929 μM | SANGER | ||
KYSE-520 | Growth Inhibition Assay | IC50=4.88018 μM | SANGER | ||
KNS-62 | Growth Inhibition Assay | IC50=4.90807 μM | SANGER | ||
ES1 | Growth Inhibition Assay | IC50=4.96035 μM | SANGER | ||
KOSC-2 | Growth Inhibition Assay | IC50=4.99959 μM | SANGER | ||
TE-9 | Growth Inhibition Assay | IC50=5.01525 μM | SANGER | ||
NCI-H1838 | Growth Inhibition Assay | IC50=5.02076 μM | SANGER | ||
KP-N-YN | Growth Inhibition Assay | IC50=5.12591 μM | SANGER | ||
ALL-PO | Growth Inhibition Assay | IC50=5.22587 μM | SANGER | ||
NOMO-1 | Growth Inhibition Assay | IC50=5.23176 μM | SANGER | ||
CGTH-W-1 | Growth Inhibition Assay | IC50=5.38584 μM | SANGER | ||
ATN-1 | Growth Inhibition Assay | IC50=5.41184 μM | SANGER | ||
AGS | Growth Inhibition Assay | IC50=5.49618 μM | SANGER | ||
SW13 | Growth Inhibition Assay | IC50=5.53265 μM | SANGER | ||
SW1990 | Growth Inhibition Assay | IC50=5.62285 μM | SANGER | ||
BFTC-905 | Growth Inhibition Assay | IC50=5.65878 μM | SANGER | ||
RMG-I | Growth Inhibition Assay | IC50=5.65942 μM | SANGER | ||
HD-MY-Z | Growth Inhibition Assay | IC50=5.68581 μM | SANGER | ||
HCC1187 | Growth Inhibition Assay | IC50=5.71032 μM | SANGER | ||
HCC2998 | Growth Inhibition Assay | IC50=5.71877 μM | SANGER | ||
RT-112 | Growth Inhibition Assay | IC50=5.90245 μM | SANGER | ||
CAKI-1 | Growth Inhibition Assay | IC50=6.00985 μM | SANGER | ||
HDLM-2 | Growth Inhibition Assay | IC50=6.01489 μM | SANGER | ||
TE-10 | Growth Inhibition Assay | IC50=6.04833 μM | SANGER | ||
KE-37 | Growth Inhibition Assay | IC50=6.07258 μM | SANGER | ||
RCM-1 | Growth Inhibition Assay | IC50=6.07719 μM | SANGER | ||
Mewo | Growth Inhibition Assay | IC50=6.11487 μM | SANGER | ||
L-428 | Growth Inhibition Assay | IC50=6.18037 μM | SANGER | ||
8-MG-BA | Growth Inhibition Assay | IC50=6.19379 μM | SANGER | ||
SK-MEL-28 | Growth Inhibition Assay | IC50=6.20967 μM | SANGER | ||
VA-ES-BJ | Growth Inhibition Assay | IC50=6.30462 μM | SANGER | ||
CAL-120 | Growth Inhibition Assay | IC50=6.45162 μM | SANGER | ||
GAMG | Growth Inhibition Assay | IC50=6.5062 μM | SANGER | ||
MSTO-221H | Growth Inhibition Assay | IC50=6.5117 μM | SANGER | ||
GCT | Growth Inhibition Assay | IC50=6.53387 μM | SANGER | ||
SH-4 | Growth Inhibition Assay | IC50=6.58844 μM | SANGER | ||
Calu-3 | Growth Inhibition Assay | IC50=6.65568 μM | SANGER | ||
SK-HEP-1 | Growth Inhibition Assay | IC50=6.71753 μM | SANGER | ||
PFSK-1 | Growth Inhibition Assay | IC50=6.73478 μM | SANGER | ||
NB12 | Growth Inhibition Assay | IC50=6.78404 μM | SANGER | ||
A388 | Growth Inhibition Assay | IC50=6.8952 μM | SANGER | ||
KLE | Growth Inhibition Assay | IC50=6.96516 μM | SANGER | ||
TE-11 | Growth Inhibition Assay | IC50=7.04967 μM | SANGER | ||
NCI-H2405 | Growth Inhibition Assay | IC50=7.08393 μM | SANGER | ||
OVCAR-4 | Growth Inhibition Assay | IC50=7.1535 μM | SANGER | ||
KP-N-YS | Growth Inhibition Assay | IC50=7.1814 μM | SANGER | ||
NOS-1 | Growth Inhibition Assay | IC50=7.25828 μM | SANGER | ||
DMS-114 | Growth Inhibition Assay | IC50=7.29631 μM | SANGER | ||
NCI-H2030 | Growth Inhibition Assay | IC50=7.33698 μM | SANGER | ||
HEL | Growth Inhibition Assay | IC50=7.37521 μM | SANGER | ||
CAL-62 | Growth Inhibition Assay | IC50=7.39866 μM | SANGER | ||
COLO-668 | Growth Inhibition Assay | IC50=7.43967 μM | SANGER | ||
SKG-IIIa | Growth Inhibition Assay | IC50=7.45381 μM | SANGER | ||
HCC1419 | Growth Inhibition Assay | IC50=7.46833 μM | SANGER | ||
OS-RC-2 | Growth Inhibition Assay | IC50=7.49894 μM | SANGER | ||
COLO-829 | Growth Inhibition Assay | IC50=7.66463 μM | SANGER | ||
NB13 | Growth Inhibition Assay | IC50=7.82667 μM | SANGER | ||
DK-MG | Growth Inhibition Assay | IC50=7.83201 μM | SANGER | ||
SHP-77 | Growth Inhibition Assay | IC50=7.86653 μM | SANGER | ||
NCI-H661 | Growth Inhibition Assay | IC50=8.05867 μM | SANGER | ||
AM-38 | Growth Inhibition Assay | IC50=8.1628 μM | SANGER | ||
VM-CUB-1 | Growth Inhibition Assay | IC50=8.17029 μM | SANGER | ||
KYSE-70 | Growth Inhibition Assay | IC50=8.19761 μM | SANGER | ||
5637 | Growth Inhibition Assay | IC50=8.31055 μM | SANGER | ||
TGBC11TKB | Growth Inhibition Assay | IC50=8.46164 μM | SANGER | ||
EGI-1 | Growth Inhibition Assay | IC50=8.60088 μM | SANGER | ||
D-392MG | Growth Inhibition Assay | IC50=8.66214 μM | SANGER | ||
A673 | Growth Inhibition Assay | IC50=8.67611 μM | SANGER | ||
COLO-792 | Growth Inhibition Assay | IC50=8.74946 μM | SANGER | ||
NCI-H1792 | Growth Inhibition Assay | IC50=8.88903 μM | SANGER | ||
LS-1034 | Growth Inhibition Assay | IC50=8.94652 μM | SANGER | ||
D-566MG | Growth Inhibition Assay | IC50=9.0181 μM | SANGER | ||
NCI-H226 | Growth Inhibition Assay | IC50=9.09 μM | SANGER | ||
NCI-H2228 | Growth Inhibition Assay | IC50=9.11081 μM | SANGER | ||
ChaGo-K-1 | Growth Inhibition Assay | IC50=9.10579 μM | SANGER | ||
RPMI-8226 | Growth Inhibition Assay | IC50=9.11304 μM | SANGER | ||
BFTC-909 | Growth Inhibition Assay | IC50=9.18297 μM | SANGER | ||
Capan-2 | Growth Inhibition Assay | IC50=9.40109 μM | SANGER | ||
HPAF-II | Growth Inhibition Assay | IC50=9.22518 μM | SANGER | ||
IA-LM | Growth Inhibition Assay | IC50=9.41966 μM | SANGER | ||
A101D | Growth Inhibition Assay | IC50=9.51719 μM | SANGER | ||
KP-4 | Growth Inhibition Assay | IC50=9.48838 μM | SANGER | ||
C32 | Growth Inhibition Assay | IC50=9.6334 μM | SANGER | ||
EFO-21 | Growth Inhibition Assay | IC50=9.58735 μM | SANGER | ||
OCI-AML2 | Growth Inhibition Assay | IC50=9.8696 μM | SANGER | ||
SW837 | Growth Inhibition Assay | IC50=9.8482 μM | SANGER | ||
NCI-H1355 | Growth Inhibition Assay | IC50=9.94088 μM | SANGER | ||
A204 | Growth Inhibition Assay | IC50=10.0466 μM | SANGER | ||
NCI-H2342 | Growth Inhibition Assay | IC50=10.0155 μM | SANGER | ||
HCE-4 | Growth Inhibition Assay | IC50=10.1122 μM | SANGER | ||
CAL-51 | Growth Inhibition Assay | IC50=10.0877 μM | SANGER | ||
DJM-1 | Growth Inhibition Assay | IC50=10.1732 μM | SANGER | ||
NCI-H810 | Growth Inhibition Assay | IC50=10.1597 μM | SANGER | ||
SK-UT-1 | Growth Inhibition Assay | IC50=10.2574 μM | SANGER | ||
YH-13 | Growth Inhibition Assay | IC50=10.3057 μM | SANGER | ||
U031 | Growth Inhibition Assay | IC50=10.2686 μM | SANGER | ||
K5 | Growth Inhibition Assay | IC50=10.3395 μM | SANGER | ||
A2058 | Growth Inhibition Assay | IC50=10.5491 μM | SANGER | ||
HEC-1 | Growth Inhibition Assay | IC50=10.4081 μM | SANGER | ||
VMRC-RCZ | Growth Inhibition Assay | IC50=10.6749 μM | SANGER | ||
SW962 | Growth Inhibition Assay | IC50=10.6204 μM | SANGER | ||
LXF-289 | Growth Inhibition Assay | IC50=10.7967 μM | SANGER | ||
D-336MG | Growth Inhibition Assay | IC50=10.7005 μM | SANGER | ||
SW900 | Growth Inhibition Assay | IC50=10.8228 μM | SANGER | ||
K-562 | Growth Inhibition Assay | IC50=10.8395 μM | SANGER | ||
SF-295 | Growth Inhibition Assay | IC50=10.9902 μM | SANGER | ||
HCC38 | Growth Inhibition Assay | IC50=10.9716 μM | SANGER | ||
LB831-BLC | Growth Inhibition Assay | IC50=11.2556 μM | SANGER | ||
FTC-133 | Growth Inhibition Assay | IC50=11.3081 μM | SANGER | ||
GOTO | Growth Inhibition Assay | IC50=11.5206 μM | SANGER | ||
HCC1954 | Growth Inhibition Assay | IC50=11.436 μM | SANGER | ||
LS-411N | Growth Inhibition Assay | IC50=11.6101 μM | SANGER | ||
NCI-H1299 | Growth Inhibition Assay | IC50=11.6647 μM | SANGER | ||
RPMI-7951 | Growth Inhibition Assay | IC50=11.6348 μM | SANGER | ||
MLMA | Growth Inhibition Assay | IC50=11.6997 μM | SANGER | ||
MMAC-SF | Growth Inhibition Assay | IC50=11.7252 μM | SANGER | ||
UM-UC-3 | Growth Inhibition Assay | IC50=11.7421 μM | SANGER | ||
HOS | Growth Inhibition Assay | IC50=11.8683 μM | SANGER | ||
SCC-9 | Growth Inhibition Assay | IC50=11.8151 μM | SANGER | ||
OE19 | Growth Inhibition Assay | IC50=11.9367 μM | SANGER | ||
Mo-T | Growth Inhibition Assay | IC50=11.9541 μM | SANGER | ||
U-118-MG | Growth Inhibition Assay | IC50=12.2441 μM | SANGER | ||
CAMA-1 | Growth Inhibition Assay | IC50=12.1633 μM | SANGER | ||
JAR | Growth Inhibition Assay | IC50=12.3369 μM | SANGER | ||
KS-1 | Growth Inhibition Assay | IC50=12.2832 μM | SANGER | ||
ABC-1 | Growth Inhibition Assay | IC50=12.341 μM | SANGER | ||
Daoy | Growth Inhibition Assay | IC50=12.4542 μM | SANGER | ||
C3A | Growth Inhibition Assay | IC50=12.5785 μM | SANGER | ||
DMS-273 | Growth Inhibition Assay | IC50=12.8633 μM | SANGER | ||
GT3TKB | Growth Inhibition Assay | IC50=12.6327 μM | SANGER | ||
RH-18 | Growth Inhibition Assay | IC50=13.2962 μM | SANGER | ||
G-361 | Growth Inhibition Assay | IC50=12.9129 μM | SANGER | ||
NCI-H1993 | Growth Inhibition Assay | IC50=13.4285 μM | SANGER | ||
SN12C | Growth Inhibition Assay | IC50=13.3808 μM | SANGER | ||
SK-PN-DW | Growth Inhibition Assay | IC50=13.8427 μM | SANGER | ||
LOXIMVI | Growth Inhibition Assay | IC50=13.6151 μM | SANGER | ||
KALS-1 | Growth Inhibition Assay | IC50=13.8525 μM | SANGER | ||
RD | Growth Inhibition Assay | IC50=14.4813 μM | SANGER | ||
A549 | Growth Inhibition Assay | IC50=14.4712 μM | SANGER | ||
LAN-6 | Growth Inhibition Assay | IC50=14.253 μM | SANGER | ||
NCI-H630 | Growth Inhibition Assay | IC50=14.9467 μM | SANGER | ||
TGBC1TKB | Growth Inhibition Assay | IC50=14.6615 μM | SANGER | ||
MIA-PaCa-2 | Growth Inhibition Assay | IC50=14.969 μM | SANGER | ||
NCI-H1755 | Growth Inhibition Assay | IC50=14.9953 μM | SANGER | ||
MOLT-4 | Growth Inhibition Assay | IC50=15.0497 μM | SANGER | ||
CW-2 | Growth Inhibition Assay | IC50=15.1421 μM | SANGER | ||
COLO-320-HSR | Growth Inhibition Assay | IC50=15.5307 μM | SANGER | ||
MCF7 | Growth Inhibition Assay | IC50=15.8145 μM | SANGER | ||
UMC-11 | Growth Inhibition Assay | IC50=15.7523 μM | SANGER | ||
NCI-H23 | Growth Inhibition Assay | IC50=15.8438 μM | SANGER | ||
HuCCT1 | Growth Inhibition Assay | IC50=15.874 μM | SANGER | ||
MPP-89 | Growth Inhibition Assay | IC50=15.9417 μM | SANGER | ||
no-11 | Growth Inhibition Assay | IC50=15.9663 μM | SANGER | ||
HT55 | Growth Inhibition Assay | IC50=15.9478 μM | SANGER | ||
BHT-101 | Growth Inhibition Assay | IC50=16.2439 μM | SANGER | ||
GP5d | Growth Inhibition Assay | IC50=16.2187 μM | SANGER | ||
D-283MED | Growth Inhibition Assay | IC50=16.4209 μM | SANGER | ||
M059J | Growth Inhibition Assay | IC50=16.284 μM | SANGER | ||
BEN | Growth Inhibition Assay | IC50=16.5155 μM | SANGER | ||
MEL-HO | Growth Inhibition Assay | IC50=16.8854 μM | SANGER | ||
LB373-MEL-D | Growth Inhibition Assay | IC50=16.7232 μM | SANGER | ||
GI-ME-N | Growth Inhibition Assay | IC50=16.9032 μM | SANGER | ||
MZ2-MEL | Growth Inhibition Assay | IC50=17.133 μM | SANGER | ||
RKO | Growth Inhibition Assay | IC50=17.0748 μM | SANGER | ||
NCI-H1581 | Growth Inhibition Assay | IC50=17.4411 μM | SANGER | ||
NCI-H1573 | Growth Inhibition Assay | IC50=17.2826 μM | SANGER | ||
NCI-H747 | Growth Inhibition Assay | IC50=17.5297 μM | SANGER | ||
SW1783 | Growth Inhibition Assay | IC50=17.6415 μM | SANGER | ||
Calu-6 | Growth Inhibition Assay | IC50=17.6782 μM | SANGER | ||
SF268 | Growth Inhibition Assay | IC50=17.6969 μM | SANGER | ||
ES8 | Growth Inhibition Assay | IC50=17.8593 μM | SANGER | ||
D-502MG | Growth Inhibition Assay | IC50=17.9808 μM | SANGER | ||
KM-H2 | Growth Inhibition Assay | IC50=17.9411 μM | SANGER | ||
SW982 | Growth Inhibition Assay | IC50=18.4075 μM | SANGER | ||
HLE | Growth Inhibition Assay | IC50=18.3148 μM | SANGER | ||
MDA-MB-361 | Growth Inhibition Assay | IC50=18.5588 μM | SANGER | ||
NCI-H1563 | Growth Inhibition Assay | IC50=18.7124 μM | SANGER | ||
MFE-280 | Growth Inhibition Assay | IC50=18.7293 μM | SANGER | ||
U251 | Growth Inhibition Assay | IC50=18.7347 μM | SANGER | ||
KNS-42 | Growth Inhibition Assay | IC50=18.8015 μM | SANGER | ||
OVCAR-8 | Growth Inhibition Assay | IC50=18.9276 μM | SANGER | ||
U-266 | Growth Inhibition Assay | IC50=18.8649 μM | SANGER | ||
MFH-ino | Growth Inhibition Assay | IC50=18.9669 μM | SANGER | ||
D-263MG | Growth Inhibition Assay | IC50=19.0172 μM | SANGER | ||
NCI-H1437 | Growth Inhibition Assay | IC50=19.0467 μM | SANGER | ||
NCI-H446 | Growth Inhibition Assay | IC50=19.3589 μM | SANGER | ||
NCI-H1048 | Growth Inhibition Assay | IC50=19.2326 μM | SANGER | ||
NCI-N87 | Growth Inhibition Assay | IC50=19.5992 μM | SANGER | ||
HuH-7 | Growth Inhibition Assay | IC50=19.7421 μM | SANGER | ||
WM-115 | Growth Inhibition Assay | IC50=19.6774 μM | SANGER | ||
NCI-H650 | Growth Inhibition Assay | IC50=19.7508 μM | SANGER | ||
TYK-nu | Growth Inhibition Assay | IC50=19.8378 μM | SANGER | ||
Becker | Growth Inhibition Assay | IC50=19.8547 μM | SANGER | ||
HGC-27 | Growth Inhibition Assay | IC50=20.1394 μM | SANGER | ||
BB49-HNC | Growth Inhibition Assay | IC50=19.92 μM | SANGER | ||
LB2518-MEL | Growth Inhibition Assay | IC50=20.3739 μM | SANGER | ||
SiHa | Growth Inhibition Assay | IC50=20.3712 μM | SANGER | ||
TE-5 | Growth Inhibition Assay | IC50=20.7482 μM | SANGER | ||
IST-SL1 | Growth Inhibition Assay | IC50=20.7879 μM | SANGER | ||
A375 | Growth Inhibition Assay | IC50=21.0567 μM | SANGER | ||
MC116 | Growth Inhibition Assay | IC50=21.0723 μM | SANGER | ||
GI-1 | Growth Inhibition Assay | IC50=21.17 μM | SANGER | ||
HOP-62 | Growth Inhibition Assay | IC50=21.2784 μM | SANGER | ||
PA-1 | Growth Inhibition Assay | IC50=21.2787 μM | SANGER | ||
HUTU-80 | Growth Inhibition Assay | IC50=21.4336 μM | SANGER | ||
HT | Growth Inhibition Assay | IC50=21.4331 μM | SANGER | ||
NCI-H1975 | Growth Inhibition Assay | IC50=21.461 μM | SANGER | ||
NCI-H1666 | Growth Inhibition Assay | IC50=1.74704 μM | SANGER | ||
COLO-678 | Growth Inhibition Assay | IC50=1.73444 μM | SANGER | ||
PANC-03-27 | Growth Inhibition Assay | IC50=1.70139 μM | SANGER | ||
BB30-HNC | Growth Inhibition Assay | IC50=1.68972 μM | SANGER | ||
ML-2 | Growth Inhibition Assay | IC50=1.64029 μM | SANGER | ||
BT-549 | Growth Inhibition Assay | IC50=1.58747 μM | SANGER | ||
HSC-3 | Growth Inhibition Assay | IC50=1.5438 μM | SANGER | ||
LAMA-84 | Growth Inhibition Assay | IC50=1.53815 μM | SANGER | ||
SCC-25 | Growth Inhibition Assay | IC50=1.52322 μM | SANGER | ||
SAS | Growth Inhibition Assay | IC50=1.51622 μM | SANGER | ||
BE-13 | Growth Inhibition Assay | IC50=1.50671 μM | SANGER | ||
J82 | Growth Inhibition Assay | IC50=1.45766 μM | SANGER | ||
697 | Growth Inhibition Assay | IC50=1.44104 μM | SANGER | ||
NCI-H526 | Growth Inhibition Assay | IC50=1.43826 μM | SANGER | ||
RH-1 | Growth Inhibition Assay | IC50=1.41136 μM | SANGER | ||
CCRF-CEM | Growth Inhibition Assay | IC50=1.4111 μM | SANGER | ||
NB5 | Growth Inhibition Assay | IC50=1.40894 μM | SANGER | ||
KMOE-2 | Growth Inhibition Assay | IC50=1.39815 μM | SANGER | ||
SK-N-DZ | Growth Inhibition Assay | IC50=1.36947 μM | SANGER | ||
SW48 | Growth Inhibition Assay | IC50=1.36618 μM | SANGER | ||
SW954 | Growth Inhibition Assay | IC50=1.34048 μM | SANGER | ||
NCI-H1650 | Growth Inhibition Assay | IC50=1.33482 μM | SANGER | ||
NKM-1 | Growth Inhibition Assay | IC50=1.32597 μM | SANGER | ||
NCI-H1092 | Growth Inhibition Assay | IC50=1.3085 μM | SANGER | ||
CTV-1 | Growth Inhibition Assay | IC50=1.308 μM | SANGER | ||
GCIY | Growth Inhibition Assay | IC50=1.30132 μM | SANGER | ||
SW1088 | Growth Inhibition Assay | IC50=1.29607 μM | SANGER | ||
769-P | Growth Inhibition Assay | IC50=1.27918 μM | SANGER | ||
OAW-42 | Growth Inhibition Assay | IC50=1.27825 μM | SANGER | ||
SNU-449 | Growth Inhibition Assay | IC50=1.22208 μM | SANGER | ||
MKN1 | Growth Inhibition Assay | IC50=1.21987 μM | SANGER | ||
NCI-H1648 | Growth Inhibition Assay | IC50=1.10616 μM | SANGER | ||
KU-19-19 | Growth Inhibition Assay | IC50=1.08541 μM | SANGER | ||
MHH-PREB-1 | Growth Inhibition Assay | IC50=1.08451 μM | SANGER | ||
EM-2 | Growth Inhibition Assay | IC50=1.03016 μM | SANGER | ||
NCI-H1304 | Growth Inhibition Assay | IC50=1.01643 μM | SANGER | ||
DOHH-2 | Growth Inhibition Assay | IC50=1.00021 μM | SANGER | ||
MS-1 | Growth Inhibition Assay | IC50=994.69 nM | SANGER | ||
SK-NEP-1 | Growth Inhibition Assay | IC50=989.44 nM | SANGER | ||
HT-3 | Growth Inhibition Assay | IC50=982.41 nM | SANGER | ||
BHY | Growth Inhibition Assay | IC50=975.48 nM | SANGER | ||
BT-474 | Growth Inhibition Assay | IC50=938.14 nM | SANGER | ||
CAPAN-1 | Growth Inhibition Assay | IC50=883.29 nM | SANGER | ||
NCI-H2126 | Growth Inhibition Assay | IC50=882.83 nM | SANGER | ||
COR-L88 | Growth Inhibition Assay | IC50=882.26 nM | SANGER | ||
DEL | Growth Inhibition Assay | IC50=877.65 nM | SANGER | ||
AU565 | Growth Inhibition Assay | IC50=869.6 nM | SANGER | ||
23132-87 | Growth Inhibition Assay | IC50=864.28 nM | SANGER | ||
LoVo | Growth Inhibition Assay | IC50=859.06 nM | SANGER | ||
TE-12 | Growth Inhibition Assay | IC50=821.11 nM | SANGER | ||
EC-GI-10 | Growth Inhibition Assay | IC50=788.52 nM | SANGER | ||
LU-135 | Growth Inhibition Assay | IC50=783.03 nM | SANGER | ||
A431 | Growth Inhibition Assay | IC50=780.04 nM | SANGER | ||
TE-6 | Growth Inhibition Assay | IC50=764.31 nM | SANGER | ||
COLO-684 | Growth Inhibition Assay | IC50=753.01 nM | SANGER | ||
HAL-01 | Growth Inhibition Assay | IC50=734.71 nM | SANGER | ||
NCI-H1770 | Growth Inhibition Assay | IC50=722.4 nM | SANGER | ||
LU-134-A | Growth Inhibition Assay | IC50=719.09 nM | SANGER | ||
L-363 | Growth Inhibition Assay | IC50=671.94 nM | SANGER | ||
ETK-1 | Growth Inhibition Assay | IC50=662.59 nM | SANGER | ||
COR-L105 | Growth Inhibition Assay | IC50=662.53 nM | SANGER | ||
NBsusSR | Growth Inhibition Assay | IC50=646.52 nM | SANGER | ||
ME-180 | Growth Inhibition Assay | IC50=632.9 nM | SANGER | ||
DBTRG-05MG | Growth Inhibition Assay | IC50=632.28 nM | SANGER | ||
MV-4-11 | Growth Inhibition Assay | IC50=627.7 nM | SANGER | ||
LB1047-RCC | Growth Inhibition Assay | IC50=625.29 nM | SANGER | ||
Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=621.46 nM | SANGER | ||
NB69 | Growth Inhibition Assay | IC50=614.35 nM | SANGER | ||
FADU | Growth Inhibition Assay | IC50=604.69 nM | SANGER | ||
NCI-H1623 | Growth Inhibition Assay | IC50=599.36 nM | SANGER | ||
CAL-39 | Growth Inhibition Assay | IC50=596.3 nM | SANGER | ||
Ca9-22 | Growth Inhibition Assay | IC50=588.64 nM | SANGER | ||
CAN | Growth Inhibition Assay | IC50=580.76 nM | SANGER | ||
RS4-11 | Growth Inhibition Assay | IC50=568.59 nM | SANGER | ||
DSH1 | Growth Inhibition Assay | IC50=566.88 nM | SANGER | ||
NB7 | Growth Inhibition Assay | IC50=546.32 nM | SANGER | ||
NCI-H82 | Growth Inhibition Assay | IC50=540.5 nM | SANGER | ||
KYSE-180 | Growth Inhibition Assay | IC50=530.62 nM | SANGER | ||
NCI-H358 | Growth Inhibition Assay | IC50=527.66 nM | SANGER | ||
SCC-15 | Growth Inhibition Assay | IC50=525.68 nM | SANGER | ||
HN | Growth Inhibition Assay | IC50=517.38 nM | SANGER | ||
TK10 | Growth Inhibition Assay | IC50=515.11 nM | SANGER | ||
MOLT-13 | Growth Inhibition Assay | IC50=514.82 nM | SANGER | ||
SK-MEL-1 | Growth Inhibition Assay | IC50=510.99 nM | SANGER | ||
HO-1-N-1 | Growth Inhibition Assay | IC50=509.25 nM | SANGER | ||
KYSE-270 | Growth Inhibition Assay | IC50=498.65 nM | SANGER | ||
BPH-1 | Growth Inhibition Assay | IC50=491.16 nM | SANGER | ||
EFO-27 | Growth Inhibition Assay | IC50=454.74 nM | SANGER | ||
DoTc2-4510 | Growth Inhibition Assay | IC50=442.12 nM | SANGER | ||
CTB-1 | Growth Inhibition Assay | IC50=424.4 nM | SANGER | ||
KY821 | Growth Inhibition Assay | IC50=408.57 nM | SANGER | ||
NUGC-3 | Growth Inhibition Assay | IC50=401.81 nM | SANGER | ||
MDA-MB-175-VII | Growth Inhibition Assay | IC50=378.88 nM | SANGER | ||
CAL-33 | Growth Inhibition Assay | IC50=370.9 nM | SANGER | ||
KASUMI-1 | Growth Inhibition Assay | IC50=366.73 nM | SANGER | ||
ECC10 | Growth Inhibition Assay | IC50=352.96 nM | SANGER | ||
A4-Fuk | Growth Inhibition Assay | IC50=350.02 nM | SANGER | ||
SK-MEL-24 | Growth Inhibition Assay | IC50=337.87 nM | SANGER | ||
HCC1806 | Growth Inhibition Assay | IC50=337.51 nM | SANGER | ||
PC-14 | Growth Inhibition Assay | IC50=333.41 nM | SANGER | ||
ACHN | Growth Inhibition Assay | IC50=331.4 nM | SANGER | ||
P12-ICHIKAWA | Growth Inhibition Assay | IC50=328.06 nM | SANGER | ||
TI-73 | Growth Inhibition Assay | IC50=312.75 nM | SANGER | ||
CAL-54 | Growth Inhibition Assay | IC50=311.23 nM | SANGER | ||
SBC-1 | Growth Inhibition Assay | IC50=307.79 nM | SANGER | ||
BALL-1 | Growth Inhibition Assay | IC50=297.42 nM | SANGER | ||
CAL-27 | Growth Inhibition Assay | IC50=289.08 nM | SANGER | ||
NCI-SNU-1 | Growth Inhibition Assay | IC50=283.32 nM | SANGER | ||
HCE-T | Growth Inhibition Assay | IC50=279.79 nM | SANGER | ||
MEG-01 | Growth Inhibition Assay | IC50=276.76 nM | SANGER | ||
CAL-72 | Growth Inhibition Assay | IC50=268.73 nM | SANGER | ||
KYSE-450 | Growth Inhibition Assay | IC50=247.92 nM | SANGER | ||
EW-13 | Growth Inhibition Assay | IC50=225.1 nM | SANGER | ||
DU-145 | Growth Inhibition Assay | IC50=219.04 nM | SANGER | ||
KYSE-140 | Growth Inhibition Assay | IC50=209.96 nM | SANGER | ||
CHL-1 | Growth Inhibition Assay | IC50=208.51 nM | SANGER | ||
KG-1 | Growth Inhibition Assay | IC50=204.34 nM | SANGER | ||
LB2241-RCC | Growth Inhibition Assay | IC50=194.93 nM | SANGER | ||
BV-173 | Growth Inhibition Assay | IC50=186.55 nM | SANGER | ||
LU-65 | Growth Inhibition Assay | IC50=166.61 nM | SANGER | ||
HSC-2 | Growth Inhibition Assay | IC50=165.57 nM | SANGER | ||
NCI-H292 | Growth Inhibition Assay | IC50=162.66 nM | SANGER | ||
H9 | Growth Inhibition Assay | IC50=137.2 nM | SANGER | ||
DOK | Growth Inhibition Assay | IC50=93.62 nM | SANGER | ||
HSC-4 | Growth Inhibition Assay | IC50=61.53 nM | SANGER | ||
DB | Growth Inhibition Assay | IC50=60.96 nM | SANGER | ||
HuO-3N1 | Growth Inhibition Assay | IC50=56.09 nM | SANGER | ||
HCC2218 | Growth Inhibition Assay | IC50=50.59 nM | SANGER | ||
EW-3 | Growth Inhibition Assay | IC50=46.04 nM | SANGER | ||
NCI-SNU-5 | Growth Inhibition Assay | IC50=28.19 nM | SANGER | ||
NCI-H720 | Growth Inhibition Assay | IC50=26.92 nM | SANGER | ||
EoL-1 | Growth Inhibition Assay | IC50=5.17 nM | SANGER | ||
A498 | Growth Inhibition Assay | Antiproliferative activity against human A498 cells expressing EGFR and SRC with IC50 of 8.6 μM | 22818848 | ||
Plasmodium falciparum | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 21817045 | |||
PC9 | Growth Inhibition Assay | Antiproliferative activity against growth-resistant human PC9 cells expressing EGFR E746_A750/T790M mutant with EC50 of 7 μM | 21208802 | ||
PC9 | Growth Inhibition Assay | Antiproliferative activity against EGFR-deficient human PC9 cells with EC50 of 0.017 μM | 21208802 | ||
KB | Growth Inhibition Assay | IC50=0.054 μM | 16516473 | ||
GAK | Growth Inhibition Assay | IC50=21.499 μM | 29795767 | ||
SK-N-AS | Growth Inhibition Assay | IC50=21.5619 μM | 19691349 | ||
OE33 | Growth Inhibition Assay | IC50=21.6046 μM | 18469809 | ||
YKG-1 | Growth Inhibition Assay | IC50=21.6545 μM | 22944119 | ||
CAL-85 | Growth Inhibition Assay | IC50=21.9305 μM | 24631359 | ||
NCI-H2347 | Growth Inhibition Assay | IC50=21.9428 μM | 28221790 | ||
PANC-08-13 | Growth Inhibition Assay | IC50=22.0119 μM | 28221790 | ||
SK-N-FI | Growth Inhibition Assay | IC50=22.3074 μM | 18469809 | ||
NEC8 | Growth Inhibition Assay | IC50=22.5078 μM | 22944119 | ||
AN3-CA | Growth Inhibition Assay | IC50=22.6084 μM | 22944119 | ||
HuO9 | Growth Inhibition Assay | IC50=22.7396 μM | 27032331 | ||
COLO-800 | Growth Inhibition Assay | IC50=22.7653 μM | 24341356 | ||
HT-29 | Growth Inhibition Assay | IC50=22.8823 μM | 21711054 | ||
OC-314 | Growth Inhibition Assay | IC50=22.8845 μM | 20873740 | ||
G-401 | Growth Inhibition Assay | IC50=23.0462 μM | 18469809 | ||
Saos-2 | Growth Inhibition Assay | IC50=23.5182 μM | 24471998 | ||
UACC-62 | Growth Inhibition Assay | IC50=23.5833 μM | 19691349 | ||
D-247MG | Growth Inhibition Assay | IC50=23.7939 μM | 18469809 | ||
COLO-741 | Growth Inhibition Assay | IC50=23.9565 μM | 20580554 | ||
ES3 | Growth Inhibition Assay | IC50=24.0023 μM | 28221790 | ||
LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=24.0211 μM | 28221790 | ||
SW1710 | Growth Inhibition Assay | IC50=24.1506 μM | 23094992 | ||
LU-99A | Growth Inhibition Assay | IC50=24.1841 μM | 17602464 | ||
HOP-92 | Growth Inhibition Assay | IC50=24.725 μM | 24471998 | ||
LS-123 | Growth Inhibition Assay | IC50=24.9614 μM | 22342146 | ||
T84 | Growth Inhibition Assay | IC50=24.9765 μM | 29328656 | ||
HCT-116 | Growth Inhibition Assay | IC50=25.4186 μM | 29471119 | ||
M14 | Growth Inhibition Assay | IC50=25.4447 μM | 17602464 | ||
OCUB-M | Growth Inhibition Assay | IC50=25.4456 μM | 21711054 | ||
MKN45 | Growth Inhibition Assay | IC50=25.6315 μM | 26025875 | ||
LCLC-97TM1 | Growth Inhibition Assay | IC50=25.7285 μM | 18588281 | ||
RVH-421 | Growth Inhibition Assay | IC50=25.8161 μM | 20873740 | ||
NKS-81-FD | Growth Inhibition Assay | IC50=25.9021 μM | 28221790 | ||
NCI-H596 | Growth Inhibition Assay | IC50=26.0487 μM | 25703296 | ||
GB-1 | Growth Inhibition Assay | IC50=26.1879 μM | 17602464 | ||
ZR-75-30 | Growth Inhibition Assay | IC50=26.2297 μM | 17602464 | ||
U-2-OS | Growth Inhibition Assay | IC50=26.3757 μM | 22342146 | ||
HuP-T3 | Growth Inhibition Assay | IC50=26.6102 μM | 21711054 | ||
MOLT-16 | Growth Inhibition Assay | IC50=26.6166 μM | 17602464 | ||
U-87-MG | Growth Inhibition Assay | IC50=26.7438 μM | 19362474 | ||
8505C | Growth Inhibition Assay | IC50=26.9126 μM | 18588281 | ||
SK-MEL-3 | Growth Inhibition Assay | IC50=26.9828 μM | 22342146 | ||
COLO-824 | Growth Inhibition Assay | IC50=27.2195 μM | 24631359 | ||
EW-1 | Growth Inhibition Assay | IC50=27.3554 μM | 29656202 | ||
UACC-257 | Growth Inhibition Assay | IC50=27.3804 μM | 28221790 | ||
Hs-578-T | Growth Inhibition Assay | IC50=27.5299 μM | 24631359 | ||
UACC-893 | Growth Inhibition Assay | IC50=27.6631 μM | 22342146 | ||
MHH-NB-11 | Growth Inhibition Assay | IC50=27.8007 μM | 20873740 | ||
KYSE-410 | Growth Inhibition Assay | IC50=28.2779 μM | 21711054 | ||
SF126 | Growth Inhibition Assay | IC50=28.7435 μM | 21711054 | ||
HT-144 | Growth Inhibition Assay | IC50=29.3362 μM | 22342146 | ||
SW1573 | Growth Inhibition Assay | IC50=29.3509 μM | 26025875 | ||
SW620 | Growth Inhibition Assay | IC50=29.3641 μM | 28075592 | ||
SCH | Growth Inhibition Assay | IC50=29.8831 μM | 20873740 | ||
EW-22 | Growth Inhibition Assay | IC50=30.1969 μM | 25703296 | ||
H4 | Growth Inhibition Assay | IC50=30.4654 μM | 26025875 | ||
CAS-1 | Growth Inhibition Assay | IC50=30.7859 μM | 24471998 | ||
MG-63 | Growth Inhibition Assay | IC50=30.8478 μM | 21711054 | ||
MDA-MB-415 | Growth Inhibition Assay | IC50=31.1753 μM | 18469809 | ||
NCI-H1395 | Growth Inhibition Assay | IC50=31.2328 μM | 19362474 | ||
Ca-Ski | Growth Inhibition Assay | IC50=31.3177 μM | 18469809 | ||
BxPC-3 | Growth Inhibition Assay | IC50=31.3729 μM | 24631359 | ||
A3-KAW | Growth Inhibition Assay | IC50=31.4471 μM | 17602464 | ||
T-24 | Growth Inhibition Assay | IC50=31.7362 μM | 20580554 | ||
NCI-H2029 | Growth Inhibition Assay | IC50=31.7765 μM | 24471998 | ||
YAPC | Growth Inhibition Assay | IC50=32.0407 μM | 21711054 | ||
SK-MEL-2 | Growth Inhibition Assay | IC50=32.052 μM | 19362474 | ||
LS-513 | Growth Inhibition Assay | IC50=32.1187 μM | 19362474 | ||
AsPC-1 | Growth Inhibition Assay | IC50=32.3605 μM | 17101674 | ||
KYSE-150 | Growth Inhibition Assay | IC50=32.3773 μM | 23230131 | ||
NCI-H520 | Growth Inhibition Assay | IC50=32.4482 μM | 21711054 | ||
JEG-3 | Growth Inhibition Assay | IC50=33.0971 μM | 23230131 | ||
GMS-10 | Growth Inhibition Assay | IC50=33.3004 μM | 21711054 | ||
HT-1080 | Growth Inhibition Assay | IC50=33.39 μM | 24195466 | ||
NCI-H1651 | Growth Inhibition Assay | IC50=33.396 μM | 19362474 | ||
NCI-H2122 | Growth Inhibition Assay | IC50=33.5574 μM | 20873740 | ||
ES5 | Growth Inhibition Assay | IC50=33.7292 μM | 29656202 | ||
8305C | Growth Inhibition Assay | IC50=33.9937 μM | 19362474 | ||
KM12 | Growth Inhibition Assay | IC50=34.0478 μM | 23230131 | ||
HCT-15 | Growth Inhibition Assay | IC50=34.127 μM | 23968824 | ||
OVCAR-5 | Growth Inhibition Assay | IC50=34.2182 μM | 24867590 | ||
NCI-H2291 | Growth Inhibition Assay | IC50=34.2472 μM | 23230131 | ||
CP50-MEL-B | Growth Inhibition Assay | IC50=34.6592 μM | 25105722 | ||
C-33-A | Growth Inhibition Assay | IC50=34.6857 μM | 27966950 | ||
NCI-H2452 | Growth Inhibition Assay | IC50=34.7882 μM | 21711054 | ||
MDA-MB-157 | Growth Inhibition Assay | IC50=34.8193 μM | 19362474 | ||
LN-405 | Growth Inhibition Assay | IC50=35.4308 μM | 20873740 | ||
MDA-MB-231 | Growth Inhibition Assay | IC50=35.5054 μM | 23360104 | ||
EW-24 | Growth Inhibition Assay | IC50=35.6335 μM | 23968824 | ||
MKN28 | Growth Inhibition Assay | IC50=35.8236 μM | 19362474 | ||
KINGS-1 | Growth Inhibition Assay | IC50=35.8434 μM | 29328656 | ||
LC-2-ad | Growth Inhibition Assay | IC50=36.699 μM | 25703296 | ||
IGR-1 | Growth Inhibition Assay | IC50=36.7075 μM | 24436994 | ||
SW626 | Growth Inhibition Assay | IC50=37.0417 μM | 22512908 | ||
ONS-76 | Growth Inhibition Assay | IC50=37.1309 μM | 23968824 | ||
T98G | Growth Inhibition Assay | IC50=37.8635 μM | 21711054 | ||
NB14 | Growth Inhibition Assay | IC50=38.4544 μM | 24436994 | ||
D-423MG | Growth Inhibition Assay | IC50=38.4869 μM | 19362474 | ||
NCI-H510A | Growth Inhibition Assay | IC50=38.6451 μM | 28495081 | ||
NMC-G1 | Growth Inhibition Assay | IC50=38.7222 μM | 21711054 | ||
SW948 | Growth Inhibition Assay | IC50=38.8949 μM | 24341356 | ||
MFM-223 | Growth Inhibition Assay | IC50=38.9431 μM | 17419604 | ||
PAN1 | Growth Inhibition Assay | IC50=38.9919 μM | 22512908 | ||
MZ7-mel | Growth Inhibition Assay | IC50=39.1199 μM | 28075592 | ||
COLO-679 | Growth Inhibition Assay | IC50=39.9708 μM | 21711054 | ||
SW872 | Growth Inhibition Assay | IC50=40.2031 μM | 24631359 | ||
HT-1197 | Growth Inhibition Assay | IC50=40.2869 μM | 27349332 | ||
ES6 | Growth Inhibition Assay | IC50=40.4552 μM | 18186604 | ||
SNU-387 | Growth Inhibition Assay | IC50=40.8238 μM | 17419604 | ||
T47D | Growth Inhibition Assay | IC50=41.0192 μM | 18186604 | ||
G-402 | Growth Inhibition Assay | IC50=41.0809 μM | 23489626 | ||
MZ1-PC | Growth Inhibition Assay | IC50=41.81 μM | 17602464 | ||
SW1417 | Growth Inhibition Assay | IC50=42.303 μM | 17602464 | ||
RERF-LC-MS | Growth Inhibition Assay | IC50=42.5087 μM | 28576633 | ||
SF539 | Growth Inhibition Assay | IC50=42.5529 μM | 23489626 | ||
ESS-1 | Growth Inhibition Assay | IC50=43.5558 μM | 28576633 | ||
RO82-W-1 | Growth Inhibition Assay | IC50=43.6153 μM | 28576633 | ||
S-117 | Growth Inhibition Assay | IC50=43.6958 μM | 22512908 | ||
SW756 | Growth Inhibition Assay | IC50=43.8242 μM | SANGER | ||
CP66-MEL | Growth Inhibition Assay | IC50=45.7143 μM | SANGER | ||
H-EMC-SS | Growth Inhibition Assay | IC50=45.7693 μM | SANGER | ||
NCI-H2052 | Growth Inhibition Assay | IC50=45.9027 μM | SANGER | ||
SW684 | Growth Inhibition Assay | IC50=47.0081 μM | SANGER | ||
HCC1569 | Growth Inhibition Assay | IC50=47.1658 μM | SANGER | ||
KGN | Growth Inhibition Assay | IC50=47.3311 μM | SANGER | ||
LCLC-103H | Growth Inhibition Assay | IC50=47.4404 μM | SANGER | ||
SW780 | Growth Inhibition Assay | IC50=47.6351 μM | SANGER | ||
NCI-H1703 | Growth Inhibition Assay | IC50=48.3352 μM | SANGER | ||
HCC1395 | Growth Inhibition Assay | IC50=48.7432 μM | SANGER | ||
點擊查看更多細胞系數據 |
產品描述 | Gefitinib是一種EGFR抑制劑,作用于NR6wtEGFR和NR6W細胞中的Tyr1173、Tyr992、Tyr1173和Tyr992,IC50 分別為37 nM、37nM、26 nM和57 nM。Gefitinib 可通過阻滯PI3K/AKT/mTOR信號通路來促進肺癌細胞的自噬和細胞凋亡。 | ||||||||
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特性 | Gefitinib是有效的EGFR酪氨酸激酶抑制劑。 | ||||||||
靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Gefitinib 作用于高和低表達EGFR的細胞系,包括NR6, NR6M 和 NR6W 細胞系,有效抑制EGFR上全部酪氨酸磷酸化位點。磷酸化位點 Tyr1173和Tyr992敏感性較低,需要高濃度Gefitinib才能抑制。Gefitinib作用于NR6W細胞,高效阻斷PLC-γ磷酸化, IC50為27nM。NR6wtEGFR 和NR6M細胞系具有低水平PLC-γ磷酸化, IC50 分別為 43 nM和 369 nM。Gefitinib抑制AKT磷酸化,作用于低EGFR和EGFRvIII表達的細胞系, IC50 分別為220 和263nM。Gefitinib按 0.1 到 0.5μM劑量處理,顯著促進而不是廢除 NR6M細胞形成集落。然而, 2μM Gefitinib 完全抑制 NR6M 集落形成。Gefitinib 作用于高和低EGFR表達的細胞系,EGF 刺激72小時后,快速抑制EGFR 和ERK 磷酸化,這種作用存在劑量依賴性。[1]Gefitinib抑制 EGF驅動的未轉化MCF10A 細胞生長,IC50為 20 nM。[2] Gefitinib 作用于MDA-MB-231細胞,抑制EGF信號。Gefitinib嚴重抑制細胞數的增多,這種作用存在劑量依賴性。 [3] |
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細胞實驗 | 細胞系 | NR6, NR6M 和 NR6W 細胞 | ||
濃度 | 0 μM -2 μM | |||
孵育時間 | 72 小時 | |||
方法 | 呈指數生長的細胞,包括 NR6, NR6M, NR6M和NR6W細胞按6倍接種在96孔板上,每孔為2000個細胞, 粘附,隨后在PBS 中清洗,然后在含0.5% FCS的培養(yǎng)基上溫育過夜。使用不同濃度(0-2 μM) Gefitinib或溶質對照DMSO 和EGF 處理細胞。誘導NR6wtEGFR和NR6W 細胞增殖的EGF最佳濃度已經測定,因此NR6wtEGFR和 NR6W 細胞中分別加入10 nM和 0.1 nM EGF。NR6 和NR6M細胞中不加入EGF。72 小時后,通過MTT 增殖檢測測量細胞數。 |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT Cyclin D1/ p16 / p27 / pRb uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP PPAR-γ | 22586683 | ||
Immunofluorescence | EGFR / LC3 PPAR-γ p-EGFR / β-catenin | 31196210 | ||
Growth inhibition assay | GI50 | 23409107 |
體內研究(In Vivo) | ||
體內研究活性 | Gefitinib 作用于無胸腺裸鼠,抑制SKOV3 或MDA-MB-231 腫瘤生長。Gefitinib高效作用于兩種類型腫瘤。處理14天后,MDA-MB-231腫瘤和SKOV3腫瘤生長抑制分別為71%和32%。 |
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動物實驗 | Animal Models | 攜帶 SKOV3或MDA-MB-231腫瘤的無胸腺裸鼠 |
Dosages | 75 mg/kg | |
Administration | 飼喂處理 |
NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
---|---|---|---|---|---|
NCT03599518 | Terminated | Non Small Cell Lung Cancer |
Daiichi Sankyo Co. Ltd.|Daiichi Sankyo |
September 21 2018 | Phase 1 |
NCT03292133 | Active not recruiting | Lung Cancer |
Massachusetts General Hospital|Novartis |
October 31 2017 | Phase 2 |
NCT03122717 | Active not recruiting | Non-Small Cell Lung Cancer |
Dana-Farber Cancer Institute|AstraZeneca |
May 9 2017 | Phase 1|Phase 2 |
NCT02932345 | Terminated | EGFR Mutation Positive Advanced Non-small-cell Lung Cancer |
AstraZeneca |
October 31 2016 | -- |
NCT02824458 | Unknown status | EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors |
Sun Yat-sen University |
June 2016 | Phase 3 |
分子量 | 446.90 | 分子式 | C22H24ClFN4O3 |
CAS號 | 184475-35-2 | SDF | Download Gefitinib SDF |
Smiles | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 89 mg/mL ( (199.14 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Ethanol : 5 mg/mL (11.18 mM) Water : Insoluble |
摩爾濃度計算器 |
體內溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
在訂購、運輸、儲存和使用我們的產品的任何階段,您遇到的任何問題,均可以通過撥打我們的熱線電話400-668-6834,或者技術支持郵箱tech@selleck.cn,直接聯(lián)系到我們。我們會在24小時內盡快聯(lián)系您。
如果有其他問題,請給我們留言。
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問題 1:
I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?
回答:
S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.