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Torin 1

Torin 1是一種有效的mTORC1/2抑制劑,在無細(xì)胞試驗(yàn)中IC50為2 nM/10 nM;作用于mTOR比作用于PI3K選擇性高1000倍。

Torin 1 Chemical Structure

Torin 1 Chemical Structure

CAS: 1222998-36-8

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mg 1419.84 現(xiàn)貨
50mg 5492.28 現(xiàn)貨
200mg 15315.3 現(xiàn)貨
1g 32678.1 現(xiàn)貨
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400-668-6834

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常與Torin 1一起在實(shí)驗(yàn)中被使用的化合物

Rapamycin


Torin 1和Rapamycin差異調(diào)節(jié)人神經(jīng)母細(xì)胞瘤細(xì)胞中鐵誘導(dǎo)的線粒體ROS的產(chǎn)生。

Huang H, et al. Biometals. 2017 Dec;30(6):975-980.

Verteporfin


Torin 1和Verteporfin聯(lián)合治療在PDX模型中產(chǎn)生最大程度的持續(xù)腫瘤生長抑制。

Dai M, et al. Nature Communications 12.1 (2021): 3055.

Chloroquine


Torin 1和Chloroquine降低BON1細(xì)胞的細(xì)胞活力并抑制細(xì)胞增殖。

Avneil-Polak S, et al. Neuroendocrinology. 2016;103(6):724-37.

Erlotinib


Torin 1可使EGFR野生型、KRAS或NRAS、p53野生型或突變型的NSCLC細(xì)胞系對Erlotinib的敏感性提高10-20倍。

Britt RR, et al.Cancer Res (2011) 71 (8_Supplement): 3780.

Cetuximab (anti-EGFR)


Torin 1和Cetuximab對OSCC異種移植小鼠的腫瘤體積生長有抑制作用。

Naruse T, et al. Oral Oncol. 2017 Feb;65:23-32.

Torin 1相關(guān)產(chǎn)品

相關(guān)信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
RPMI-8402 Growth Inhibition Assay IC50=0.07789 μM SANGER
HAL-01 Growth Inhibition Assay IC50=0.07658 μM SANGER
KM12 Growth Inhibition Assay IC50=0.0764 μM SANGER
PF-382 Growth Inhibition Assay IC50=0.07569 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.07549 μM SANGER
ARH-77 Growth Inhibition Assay IC50=0.07278 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=0.07212 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.07173 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.06995 μM SANGER
A388 Growth Inhibition Assay IC50=0.06893 μM SANGER
MLMA Growth Inhibition Assay IC50=0.0678 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=0.06605 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=0.06598 μM SANGER
KLE Growth Inhibition Assay IC50=0.06584 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.06548 μM SANGER
Becker Growth Inhibition Assay IC50=0.0642 μM SANGER
K5 Growth Inhibition Assay IC50=0.06403 μM SANGER
LOUCY Growth Inhibition Assay IC50=0.06394 μM SANGER
SR Growth Inhibition Assay IC50=0.06374 μM SANGER
SNB75 Growth Inhibition Assay IC50=0.06341 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.06225 μM SANGER
LS-123 Growth Inhibition Assay IC50=0.05942 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.05938 μM SANGER
HC-1 Growth Inhibition Assay IC50=0.05827 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=0.05803 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=0.05799 μM SANGER
SW962 Growth Inhibition Assay IC50=0.05763 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.0573 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=0.05362 μM SANGER
NB6 Growth Inhibition Assay IC50=0.05271 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.04956 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=0.04949 μM SANGER
HCC1599 Growth Inhibition Assay IC50=0.04879 μM SANGER
NB13 Growth Inhibition Assay IC50=0.04776 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.04629 μM SANGER
COLO-684 Growth Inhibition Assay IC50=0.04561 μM SANGER
TE-15 Growth Inhibition Assay IC50=0.04435 μM SANGER
SF126 Growth Inhibition Assay IC50=0.04361 μM SANGER
SW982 Growth Inhibition Assay IC50=0.04246 μM SANGER
Daudi Growth Inhibition Assay IC50=0.04225 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=0.04188 μM SANGER
TK10 Growth Inhibition Assay IC50=0.04019 μM SANGER
LC-1F Growth Inhibition Assay IC50=0.03989 μM SANGER
HCE-4 Growth Inhibition Assay IC50=0.03855 μM SANGER
TE-5 Growth Inhibition Assay IC50=0.03854 μM SANGER
SW954 Growth Inhibition Assay IC50=0.0379 μM SANGER
CP67-MEL Growth Inhibition Assay IC50=0.03759 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.03759 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.03691 μM SANGER
EB-3 Growth Inhibition Assay IC50=0.03643 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.03622 μM SANGER
SH-4 Growth Inhibition Assay IC50=0.03582 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.03556 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.03448 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=0.03371 μM SANGER
TE-10 Growth Inhibition Assay IC50=0.03311 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.03226 μM SANGER
GAK Growth Inhibition Assay IC50=0.03186 μM SANGER
CESS Growth Inhibition Assay IC50=0.03099 μM SANGER
ES1 Growth Inhibition Assay IC50=0.03097 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=0.03094 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.02996 μM SANGER
IA-LM Growth Inhibition Assay IC50=0.02917 μM SANGER
LXF-289 Growth Inhibition Assay IC50=0.02872 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=0.02871 μM SANGER
DEL Growth Inhibition Assay IC50=0.02815 μM SANGER
MFH-ino Growth Inhibition Assay IC50=0.02812 μM SANGER
ATN-1 Growth Inhibition Assay IC50=0.02789 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=0.0275 μM SANGER
MC116 Growth Inhibition Assay IC50=0.0268 μM SANGER
GR-ST Growth Inhibition Assay IC50=0.02655 μM SANGER
A101D Growth Inhibition Assay IC50=0.0265 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=0.02633 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=0.02609 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.0255 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=0.02488 μM SANGER
GI-1 Growth Inhibition Assay IC50=0.02469 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=0.02426 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=0.02414 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.02372 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=0.02337 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=0.0233 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.02323 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=0.02261 μM SANGER
SW872 Growth Inhibition Assay IC50=0.02247 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.02203 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.02167 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.02137 μM SANGER
ES8 Growth Inhibition Assay IC50=0.01844 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=0.01818 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=0.01774 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.01646 μM SANGER
HEL Growth Inhibition Assay IC50=0.0164 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.01622 μM SANGER
no-10 Growth Inhibition Assay IC50=0.01584 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.01573 μM SANGER
GB-1 Growth Inhibition Assay IC50=0.01553 μM SANGER
CMK Growth Inhibition Assay IC50=0.01543 μM SANGER
RKO Growth Inhibition Assay IC50=0.01533 μM SANGER
ACN Growth Inhibition Assay IC50=0.015 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.01451 μM SANGER
LS-411N Growth Inhibition Assay IC50=0.01439 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=0.01413 μM SANGER
PSN1 Growth Inhibition Assay IC50=0.01409 μM SANGER
no-11 Growth Inhibition Assay IC50=0.01395 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.01392 μM SANGER
KGN Growth Inhibition Assay IC50=0.01359 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=0.01319 μM SANGER
KU812 Growth Inhibition Assay IC50=0.01296 μM SANGER
OPM-2 Growth Inhibition Assay IC50=0.0129 μM SANGER
KALS-1 Growth Inhibition Assay IC50=0.01198 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.01192 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=0.01137 μM SANGER
NALM-6 Growth Inhibition Assay IC50=0.01102 μM SANGER
ES6 Growth Inhibition Assay IC50=0.01083 μM SANGER
GCIY Growth Inhibition Assay IC50=0.01007 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=0.00984 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=0.00929 μM SANGER
EVSA-T Growth Inhibition Assay IC50=0.00892 μM SANGER
EW-1 Growth Inhibition Assay IC50=0.00749 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=0.00707 μM SANGER
BL-41 Growth Inhibition Assay IC50=0.00696 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=0.00651 μM SANGER
697 Growth Inhibition Assay IC50=0.00634 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=0.00379 μM SANGER
BL-70 Growth Inhibition Assay IC50=0.00337 μM SANGER
RL95-2 Growth Inhibition Assay IC50=0.0032 μM SANGER
L-363 Growth Inhibition Assay IC50=0.00284 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.00242 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=0.00225 μM SANGER
OCUB-M Growth Inhibition Assay IC50=0.00194 μM SANGER
ETK-1 Growth Inhibition Assay IC50=0.000306 μM SANGER
OMC-1 Growth Inhibition Assay IC50=0.07804 μM SANGER
HT Growth Inhibition Assay IC50=0.08 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.08055 μM SANGER
KNS-42 Growth Inhibition Assay IC50=0.08203 μM SANGER
BC-3 Growth Inhibition Assay IC50=0.08204 μM SANGER
ES4 Growth Inhibition Assay IC50=0.08296 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=0.0844 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.08696 μM SANGER
LC4-1 Growth Inhibition Assay IC50=0.08738 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.08904 μM SANGER
LP-1 Growth Inhibition Assay IC50=0.08938 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.09016 μM SANGER
K-562 Growth Inhibition Assay IC50=0.0912 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.09153 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.09165 μM SANGER
RXF393 Growth Inhibition Assay IC50=0.09462 μM SANGER
NB5 Growth Inhibition Assay IC50=0.09625 μM SANGER
A704 Growth Inhibition Assay IC50=0.09741 μM SANGER
SF268 Growth Inhibition Assay IC50=0.09825 μM SANGER
UACC-257 Growth Inhibition Assay IC50=0.09833 μM SANGER
L-428 Growth Inhibition Assay IC50=0.1032 μM SANGER
ST486 Growth Inhibition Assay IC50=0.10606 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.10709 μM SANGER
COR-L279 Growth Inhibition Assay IC50=0.10832 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=0.10843 μM SANGER
GT3TKB Growth Inhibition Assay IC50=0.10918 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.1094 μM SANGER
SBC-1 Growth Inhibition Assay IC50=0.11119 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=0.11273 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=0.11394 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.11529 μM SANGER
JAR Growth Inhibition Assay IC50=0.11598 μM SANGER
NB17 Growth Inhibition Assay IC50=0.11652 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=0.11705 μM SANGER
CAL-148 Growth Inhibition Assay IC50=0.118 μM SANGER
K052 Growth Inhibition Assay IC50=0.11851 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=0.12233 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=0.12432 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=0.12515 μM SANGER
SCC-3 Growth Inhibition Assay IC50=0.12851 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.12975 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=0.13086 μM SANGER
ONS-76 Growth Inhibition Assay IC50=0.1313 μM SANGER
U-266 Growth Inhibition Assay IC50=0.13245 μM SANGER
HH Growth Inhibition Assay IC50=0.13535 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=0.13587 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=0.13596 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=0.13746 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.13953 μM SANGER
SCH Growth Inhibition Assay IC50=0.13974 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=0.14104 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=0.14252 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=0.14719 μM SANGER
HL-60 Growth Inhibition Assay IC50=0.1492 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=0.15539 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=0.16076 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.16101 μM SANGER
IMR-5 Growth Inhibition Assay IC50=0.16483 μM SANGER
Calu-6 Growth Inhibition Assay IC50=0.16537 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=0.16728 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=0.16891 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=0.1802 μM SANGER
MPP-89 Growth Inhibition Assay IC50=0.18121 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.18436 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.18628 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=0.18911 μM SANGER
COLO-829 Growth Inhibition Assay IC50=0.20673 μM SANGER
GOTO Growth Inhibition Assay IC50=0.2073 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.21718 μM SANGER
KY821 Growth Inhibition Assay IC50=0.22045 μM SANGER
CTB-1 Growth Inhibition Assay IC50=0.22228 μM SANGER
TALL-1 Growth Inhibition Assay IC50=0.22921 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.22962 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=0.2351 μM SANGER
DMS-114 Growth Inhibition Assay IC50=0.23993 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=0.24316 μM SANGER
DG-75 Growth Inhibition Assay IC50=0.26195 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.26557 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=0.27538 μM SANGER
NB1 Growth Inhibition Assay IC50=0.27926 μM SANGER
RH-1 Growth Inhibition Assay IC50=0.27989 μM SANGER
TE-1 Growth Inhibition Assay IC50=0.28479 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=0.2884 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.28985 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.29334 μM SANGER
COLO-668 Growth Inhibition Assay IC50=0.29429 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=0.29689 μM SANGER
MN-60 Growth Inhibition Assay IC50=0.29905 μM SANGER
L-540 Growth Inhibition Assay IC50=0.30081 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.30183 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=0.30205 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=0.30331 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=0.31415 μM SANGER
NB69 Growth Inhibition Assay IC50=0.32188 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=0.33036 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=0.33468 μM SANGER
HCC2157 Growth Inhibition Assay IC50=0.33954 μM SANGER
LS-1034 Growth Inhibition Assay IC50=0.36388 μM SANGER
BOKU Growth Inhibition Assay IC50=0.37199 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.37234 μM SANGER
TGW Growth Inhibition Assay IC50=0.37453 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=0.38215 μM SANGER
LS-513 Growth Inhibition Assay IC50=0.39071 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=0.39971 μM SANGER
MS-1 Growth Inhibition Assay IC50=0.40177 μM SANGER
EKVX Growth Inhibition Assay IC50=0.44461 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=0.464 μM SANGER
HCC1187 Growth Inhibition Assay IC50=0.46768 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.47227 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=0.4784 μM SANGER
DB Growth Inhibition Assay IC50=0.50055 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.50247 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=0.50697 μM SANGER
CA46 Growth Inhibition Assay IC50=0.50917 μM SANGER
EHEB Growth Inhibition Assay IC50=0.51193 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.54321 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.54962 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.55296 μM SANGER
MC-CAR Growth Inhibition Assay IC50=0.55431 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.56172 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=0.58748 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=0.6258 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=0.64526 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=0.64883 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=0.6535 μM SANGER
D-263MG Growth Inhibition Assay IC50=0.66101 μM SANGER
TE-6 Growth Inhibition Assay IC50=0.68104 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=0.69711 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=0.77236 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.78235 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=0.85825 μM SANGER
COLO-824 Growth Inhibition Assay IC50=0.87835 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=0.90958 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=0.96657 μM SANGER
SF539 Growth Inhibition Assay IC50=0.98396 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.98663 μM SANGER
A253 Growth Inhibition Assay IC50=0.98885 μM SANGER
TE-441-T Growth Inhibition Assay IC50=1.0435 μM SANGER
COR-L88 Growth Inhibition Assay IC50=1.11354 μM SANGER
CPC-N Growth Inhibition Assay IC50=1.15888 μM SANGER
NCI-H2107 Growth Inhibition Assay IC50=1.17261 μM SANGER
ECC4 Growth Inhibition Assay IC50=1.18693 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=1.19299 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=1.32928 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=1.3304 μM SANGER
LU-165 Growth Inhibition Assay IC50=1.45467 μM SANGER
Raji Growth Inhibition Assay IC50=1.47259 μM SANGER
EW-24 Growth Inhibition Assay IC50=1.54619 μM SANGER
KP-N-RT-BM-1 Growth Inhibition Assay IC50=1.56551 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=1.64877 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=1.66651 μM SANGER
SIMA Growth Inhibition Assay IC50=1.68233 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=1.70765 μM SANGER
REH Growth Inhibition Assay IC50=1.71078 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=1.93551 μM SANGER
DMS-153 Growth Inhibition Assay IC50=1.9759 μM SANGER
NB10 Growth Inhibition Assay IC50=2.20878 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=2.61905 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=2.75381 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=2.95394 μM SANGER
KM-H2 Growth Inhibition Assay IC50=3.65396 μM SANGER
KG-1 Growth Inhibition Assay IC50=3.71688 μM SANGER
D-283MED Growth Inhibition Assay IC50=3.7587 μM SANGER
LU-65 Growth Inhibition Assay IC50=4.11485 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=4.18898 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=4.29174 μM SANGER
D-247MG Growth Inhibition Assay IC50=4.43191 μM SANGER
P31-FUJ Growth Inhibition Assay IC50=4.45019 μM SANGER
DMS-79 Growth Inhibition Assay IC50=4.93183 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=4.97509 μM SANGER
JVM-3 Growth Inhibition Assay IC50=5.25014 μM SANGER
LAN-6 Growth Inhibition Assay IC50=5.51736 μM SANGER
DJM-1 Growth Inhibition Assay IC50=5.56029 μM SANGER
JVM-2 Growth Inhibition Assay IC50=5.67092 μM SANGER
U-87-MG Growth Inhibition Assay IC50=5.89964 μM SANGER
SHP-77 Growth Inhibition Assay IC50=5.94928 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=6.27013 μM SANGER
ES7 Growth Inhibition Assay IC50=6.39924 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=6.51609 μM SANGER
CAS-1 Growth Inhibition Assay IC50=7.09749 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=8.23152 μM SANGER
ES5 Growth Inhibition Assay IC50=9.52286 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=9.95902 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=10.5927 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=11.3718 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=12.2699 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=13.3195 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=13.3221 μM SANGER
SW684 Growth Inhibition Assay IC50=13.9797 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=15.0447 μM SANGER
EW-13 Growth Inhibition Assay IC50=15.2021 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=15.8644 μM SANGER
CHP-126 Growth Inhibition Assay IC50=17.1918 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=18.0403 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=20.1848 μM SANGER
EW-11 Growth Inhibition Assay IC50=24.2718 μM SANGER
EB2 Growth Inhibition Assay IC50=31.5318 μM SANGER
D-502MG Growth Inhibition Assay IC50=43.9229 μM SANGER
U-698-M Growth Inhibition Assay IC50=48.8671 μM SANGER
ES3 Growth Inhibition Assay IC50=49.3893 μM SANGER
PC3 Function assay Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting, EC50 = 1.8 μM. 21322566
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
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生物活性

產(chǎn)品描述 Torin 1是一種有效的mTORC1/2抑制劑,在無細(xì)胞試驗(yàn)中IC50為2 nM/10 nM;作用于mTOR比作用于PI3K選擇性高1000倍。
靶點(diǎn)
mTORC1 [1]
(Cell-free assay)
mTOR [2]
(Cell-free assay)
DNA-PK [2]
(Cell-free assay)
mTORC2 [1]
(Cell-free assay)
p110γ [2]
(Cell-free assay)
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2 nM 4.32 nM 6.34 nM 10 nM 171 nM
體外研究(In Vitro)
體外研究活性 Torin1在2和10 nM濃度下分別抑制mTORC1 和mTORC2底物的磷酸化。此外,Torin1對mTOR比對PI3K (EC50 = 1800 nM)的選擇性高1000倍,比對450種其它蛋白激酶的結(jié)合選擇性高100倍。[1] [2] Torin1通過耐rapamycin機(jī)制引起細(xì)胞周期阻滯,并且其不依賴于mTORC2。Torin1比rapamycin更完全地干擾mTORC1依賴表現(xiàn)型。Cap依賴性翻譯需要mTORC1耐Rapamycin的功能。[1]在近期的一項(xiàng)研究中,據(jù)報(bào)道Torin1通過活化人內(nèi)分泌細(xì)胞系BON 中MEK/ERK/c-Jun通路,能夠增加神經(jīng)降壓素分泌和基因表達(dá)。[3]
激酶實(shí)驗(yàn) mTORC1和 mTORC2體外激酶試驗(yàn)
為產(chǎn)生可溶性mTORC1,HEK-293T細(xì)胞系,穩(wěn)定表達(dá)N端FLAG標(biāo)記的Raptor,使用水泡性口炎病毒G-假型病毒MSCV逆轉(zhuǎn)錄酶病毒產(chǎn)生。對于mTORC2,產(chǎn)生相似的HeLa細(xì)胞,能夠穩(wěn)定表達(dá)N端FLAG-標(biāo)記的Protor-1。兩個(gè)復(fù)合物通過在50 mm HEPES,pH 7.4,10 mm 焦磷酸鈉,10 mm β-甘油磷酸鈉,100 mm NaCl,2 mm EDTA,0.3% CHAPS中裂解細(xì)胞純化。細(xì)胞在4 °C下裂解30分鐘,不溶解部分通過以13,000 rpm微量離心10分鐘移除。上清液與FLAG-M2單克隆抗體-瓊脂糖培育1小時(shí),然后用裂解緩沖液洗滌3次,用包含終濃度0.5 M NaCl的裂解緩沖液洗滌1次。純化的mTORC1用100 μg/mL 3×FLAG多肽在50 mm HEPES,pH 7.4,100 mm NaCl中洗脫。將洗出液等分收集,儲存在-80 °C。純化底物S6K1 和 Akt1。激酶試驗(yàn)在30 °C,由激酶緩沖液(25 mm HEPES,pH 7.4,50 mm KCl,10 mm MgCl2,500 μm ATP)和150 ng 滅活的S6K1或Akt1底物組成的20 μL終體積混合物中進(jìn)行。反應(yīng)通過加入80 μL樣品緩沖液停止,并沸煮5分鐘。隨后,樣品通過SDS-PAGE和免疫印跡法分析。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MEFs
濃度 ~250 nM
孵育時(shí)間 4天
方法 細(xì)胞活性通過CellTiter-Glo發(fā)光法細(xì)胞活性測定評估。在第0天,細(xì)胞以500細(xì)胞每孔接種到96孔板,并生長過夜。第1天,細(xì)胞用適當(dāng)?shù)幕衔锾幚?,隨后在第3-5天分析。對于分析,板在室溫下培育60分鐘,將50 μL CellTiter-Glo試劑加入每孔中,板在定軌搖床上混合12分鐘。發(fā)光在標(biāo)準(zhǔn)平板光度計(jì)上定量。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot Vinculin / p-S6 p-mTOR(S2481) / mTOR / rictor / Sin1 / p-Akt S473 / p-Akt T450 / p-Akt T308 / p-S6K1 T389 / S6K1 LC3 / p62 / PARP / pAKT(S473) / p4EBP1(S65) / pS6K1(T389) / pS6(S235/236) ATF4 / p-S6K(T389) / S6K / p-eIF2α(S51) / eIF2α / 4EBP1 / eIF3b 28757207
Immunofluorescence lipin-1 28347999
Growth inhibition assay Cell viability 28757207
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Torin1在20 mg/kg劑量下,在U87MG異種移植模型中是有效的,并且在腫瘤和外周組織中對mTOR下游效應(yīng)蛋白表現(xiàn)出良好的藥效學(xué)抑制作用。[2]
動物實(shí)驗(yàn) Animal Models U87MG 異種移植物模型
Dosages 20 mg/kg
Administration 腹腔注射給藥,每天一次

化學(xué)信息&溶解度

分子量 607.62 分子式

C35H28F3N5O2

CAS號 1222998-36-8 SDF Download Torin 1 SDF
Smiles CCC(=O)N1CCN(CC1)C2=C(C=C(C=C2)N3C(=O)C=CC4=CN=C5C=CC(=CC5=C43)C6=CC7=CC=CC=C7N=C6)C(F)(F)F
儲存條件(自收到貨起)

體外溶解度
批次:

DMSO : 3 mg/mL ( (4.93 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次:

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(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器(澄清溶液)

第一步:請輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)過程中的損耗,建議多配一只動物的藥量)

mg/kg g μL

第二步:請輸入動物體內(nèi)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)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)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,:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);

體內(nèi)配方配制方法: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(nèi)配方配制方法: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(jìn)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。

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常見問題及建議解決方法

問題 1:
How to re-constitute the inhibitor for i.p. administration?

回答:
S2827 Torin 1 can be dissolved in 5% DMSO/30% PEG 300/ddH2O at 0.25 mg/ml clearly, and in 10% DMSO/corn oil at 0.5 mg/ml, it is also a clear solution.

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