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Cyclopamine

別名: 11-deoxojervine 中文名稱：環(huán)巴胺

Cyclopamine (11-deoxojervine)是一種特異性Hedgehog (Hh)信號(hào)通路拮抗劑，作用于Smoothened (Smo)，在TM3Hh12細(xì)胞中IC50為46 nM。

Cyclopamine Chemical Structure

Cyclopamine Chemical Structure

CAS: 4449-51-8

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
5mg 1227.56 現(xiàn)貨
25mg 3037.37 現(xiàn)貨
50mg 3833.48 現(xiàn)貨
1g 22113 現(xiàn)貨
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Cyclopamine相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothened信號(hào)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
DU145 Growth inhibition assay 5 uM 96 hrs Growth inhibition of human DU145 cells at 5 uM after 96 hrs 18249125
DU145 Growth inhibition assay 10 uM 96 hrs Growth inhibition of human DU145 cells at 10 uM after 96 hrs 18249125
PANC1 Function assay 0.2 uM 24 hrs Inhibition of Hh/GLI1-mediated PTCH mRNA expression in human PANC1 cells at 0.2 uM after 24 hrs by RT-PCR 20450170
PANC1 Function assay 0.4 uM 24 hrs Inhibition of Hh/GLI1-mediated PTCH mRNA expression in human PANC1 cells at 0.4 uM after 24 hrs by RT-PCR 20450170
Shh Light2 Function assay 6.25 uM 30 hrs Inhibition of N-palmitoylated Shh in mouse Shh Light2 cells at 6.25 uM after 30 hrs by firefly luciferase reporter gene assay 19151731
U87MG Function assay 10 uM 4 hrs Inhibition of Hedgehog signaling pathway in human U87MG cells assessed as down regulation of Gli1 at 10 uM after 4 hrs by RT-PCR analysis 22226657
HEK293 Function assay 5 uM 10 hrs Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells at 5 uM measured after 10 hrs by DAPI staining based fluorescence microscopic assay 27736063
HEK293 Function assay 5 uM 10 hrs Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells at 5 uM measured after 10 hrs by FACS analysis 27736063
U2OS Function assay 5 uM 6 hrs Antagonist activity at chimeric Smo 633 mutant expressed in U2OS cells coexpressing beta arrestin2-GFP assessed as inhibition of intracellular beta arrestin2-GFP aggregate formation at 5 uM after 6 hrs by confocal microscopy 23063522
C3H10T1/2 Function assay 55.5 to 4500 nM Competitive inhibition of Smo in mouse C3H10T1/2 cells assessed as inhibition of SAG-induced Gli1 transcriptional activity at 55.5 to 4500 nM by qPCR analysis 23074541
U2OS Function assay 2 hrs Displacement of [3H]cyclopamine from wild type Smo expressed in U2OS cells after 2 hrs by scintillation counting, Ki = 0.0127 μM. 23063522
TM3 Function assay 48 hrs Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay, IC50 = 0.046 μM. 19091559
HEK293 Function assay 2 hrs Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy, IC50 = 0.064 μM. 22268551
Shh Light2 Function assay 30 hrs Inhibition of hedgehog signaling pathway in mouse Shh Light2 cells assessed as inhibition of sonic hedgehog-induced GLI1-mediated transcriptional activity measured after 30 hrs by dual luciferase reporter gene assay, IC50 = 0.0741 μM. 27567371
DaOY Function assay 48 hrs Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis, IC50 = 0.16 μM. 24900716
U2OS Function assay 2 hrs Displacement of [3H]cyclopamine from Smo D473H mutant expressed in U2OS cells after 2 hrs by scintillation counting, Ki = 0.232 μM. 23063522
Shh Light2 Function assay 40 hrs Inhibition of SHH pathway in mouse Shh Light2 cells after 40 hrs by Gli-dependent luciferase reporter gene assay, IC50 = 0.3 μM. 21592788
M210B4 Function assay 24 hrs Inhibition of Hedgehog signaling in mouse M210B4 cells assessed as downregulation of Ptch mRNA expression after 24 hrs by RT-PCR analysis, IC50 = 0.43 μM. 24900716
Shh-Light 2 Function assay 2 days Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method, IC50 = 0.484 μM. 23063522
C3H10T1/2 Function assay 6 hrs Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs, IC50 = 0.62 μM. 22268551
ASZ001 Function assay 48 hrs Inhibition of Hedgehog signaling in mouse ASZ001 cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis, IC50 = 0.66 μM. 24900716
M210B4 Function assay 24 hrs Inhibition of Hedgehog signaling in mouse M210B4 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by RT-PCR analysis, IC50 = 0.8 μM. 24900716
Shh-Light2 Function assay 48 hrs Inhibition of SHH in mouse Shh-Light2 cells after 48 hrs by Gli1 reporter gene assay in presence of SAG, IC50 = 1.312 μM. 19541490
MEF Function assay 30 hrs Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli-responsive betagalactosidase activity after 30 hrs by BetaGLo assay, IC50 = 1.9 μM. 23074541
U87MG Antiproliferative assay 72 hrs Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay, IC50 = 22.5 μM. 22226657
KALS-1 Growth Inhibition Assay IC50=115.941 μM SANGER
NCCIT Growth Inhibition Assay IC50=112.529 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=110.976 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=108.784 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=104.986 μM SANGER
KS-1 Growth Inhibition Assay IC50=101.639 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=100.789 μM SANGER
BV-173 Growth Inhibition Assay IC50=100.325 μM SANGER
GCIY Growth Inhibition Assay IC50=99.0954 μM SANGER
BE-13 Growth Inhibition Assay IC50=99.0477 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=84.6992 μM SANGER
HCC1599 Growth Inhibition Assay IC50=84.2837 μM SANGER
LP-1 Growth Inhibition Assay IC50=82.8731 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=76.9369 μM SANGER
D-247MG Growth Inhibition Assay IC50=73.5442 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=73.4705 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=72.8441 μM SANGER
D-542MG Growth Inhibition Assay IC50=68.4135 μM SANGER
KE-37 Growth Inhibition Assay IC50=66.2668 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=63.5657 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=60.6538 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=60.5493 μM SANGER
GI-1 Growth Inhibition Assay IC50=56.6149 μM SANGER
DJM-1 Growth Inhibition Assay IC50=56.3391 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=53.5884 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=53.3923 μM SANGER
ML-2 Growth Inhibition Assay IC50=52.9195 μM SANGER
D-502MG Growth Inhibition Assay IC50=51.6271 μM SANGER
CTV-1 Growth Inhibition Assay IC50=51.074 μM SANGER
MS-1 Growth Inhibition Assay IC50=50.9351 μM SANGER
RS4-11 Growth Inhibition Assay IC50=49.0938 μM SANGER
CESS Growth Inhibition Assay IC50=44.2232 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=42.7074 μM SANGER
A388 Growth Inhibition Assay IC50=42.5848 μM SANGER
LC4-1 Growth Inhibition Assay IC50=40.8716 μM SANGER
no-11 Growth Inhibition Assay IC50=40.5521 μM SANGER
D-392MG Growth Inhibition Assay IC50=40.2215 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=38.224 μM SANGER
BC-1 Growth Inhibition Assay IC50=37.9746 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=34.3306 μM SANGER
NOS-1 Growth Inhibition Assay IC50=34.2956 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=32.5211 μM SANGER
L-363 Growth Inhibition Assay IC50=31.7461 μM SANGER
ATN-1 Growth Inhibition Assay IC50=31.2329 μM SANGER
EVSA-T Growth Inhibition Assay IC50=27.5561 μM SANGER
COLO-829 Growth Inhibition Assay IC50=26.8483 μM SANGER
697 Growth Inhibition Assay IC50=26.6155 μM SANGER
SR Growth Inhibition Assay IC50=23.6715 μM SANGER
DEL Growth Inhibition Assay IC50=20.1471 μM SANGER
NALM-6 Growth Inhibition Assay IC50=19.0167 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=18.5948 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=15.8537 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=13.1123 μM SANGER
ALL-PO Growth Inhibition Assay IC50=11.7734 μM SANGER
LS-513 Growth Inhibition Assay IC50=11.3547 μM SANGER
no-10 Growth Inhibition Assay IC50=9.9039 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=9.35689 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=5.8666 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=116.679 μM SANGER
HH Growth Inhibition Assay IC50=117.395 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=118.488 μM SANGER
EB-3 Growth Inhibition Assay IC50=123.094 μM SANGER
BL-70 Growth Inhibition Assay IC50=123.127 μM SANGER
K-562 Growth Inhibition Assay IC50=126.245 μM SANGER
HT-144 Growth Inhibition Assay IC50=133.164 μM SANGER
PF-382 Growth Inhibition Assay IC50=134.361 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=135.045 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=135.587 μM SANGER
LXF-289 Growth Inhibition Assay IC50=139.781 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=142.932 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=147.13 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=149.12 μM SANGER
GB-1 Growth Inhibition Assay IC50=149.322 μM SANGER
CMK Growth Inhibition Assay IC50=149.515 μM SANGER
MPP-89 Growth Inhibition Assay IC50=156.035 μM SANGER
KU812 Growth Inhibition Assay IC50=161.902 μM SANGER
REH Growth Inhibition Assay IC50=162.125 μM SANGER
NEC8 Growth Inhibition Assay IC50=165.026 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=168.395 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=169.915 μM SANGER
Becker Growth Inhibition Assay IC50=174.18 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=175.845 μM SANGER
LU-139 Growth Inhibition Assay IC50=178.019 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=179.646 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=179.996 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=182.85 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=187.969 μM SANGER
KMS-12-PE Growth Inhibition Assay IC50=189.273 μM SANGER
Daudi Growth Inhibition Assay IC50=191.128 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=191.699 μM SANGER
NCI-H2107 Growth Inhibition Assay IC50=193.739 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=194.719 μM SANGER
MC-CAR Growth Inhibition Assay IC50=202.253 μM SANGER
SNB75 Growth Inhibition Assay IC50=221.94 μM SANGER
ES4 Growth Inhibition Assay IC50=223.783 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=228.352 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=229.489 μM SANGER
ES6 Growth Inhibition Assay IC50=239.43 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=241.197 μM SANGER
JAR Growth Inhibition Assay IC50=256.225 μM SANGER
NB1 Growth Inhibition Assay IC50=260.516 μM SANGER
D-336MG Growth Inhibition Assay IC50=260.698 μM SANGER
BC-3 Growth Inhibition Assay IC50=265.178 μM SANGER
HCC2218 Growth Inhibition Assay IC50=266.415 μM SANGER
TE-9 Growth Inhibition Assay IC50=266.627 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=266.753 μM SANGER
CTB-1 Growth Inhibition Assay IC50=269.973 μM SANGER
NB7 Growth Inhibition Assay IC50=271 μM SANGER
ST486 Growth Inhibition Assay IC50=277.412 μM SANGER
HCC1187 Growth Inhibition Assay IC50=282.811 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=284.248 μM SANGER
COR-L279 Growth Inhibition Assay IC50=291.584 μM SANGER
ES8 Growth Inhibition Assay IC50=294.182 μM SANGER
U-698-M Growth Inhibition Assay IC50=298.243 μM SANGER
HEL Growth Inhibition Assay IC50=309.149 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=310.674 μM SANGER
KY821 Growth Inhibition Assay IC50=336.595 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=345.618 μM SANGER
LS-411N Growth Inhibition Assay IC50=354.66 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=359.782 μM SANGER
HT Growth Inhibition Assay IC50=367.711 μM SANGER
HC-1 Growth Inhibition Assay IC50=367.787 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=372.934 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=376.245 μM SANGER
HAL-01 Growth Inhibition Assay IC50=379.838 μM SANGER
ARH-77 Growth Inhibition Assay IC50=394.008 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=397.233 μM SANGER
SIMA Growth Inhibition Assay IC50=403.933 μM SANGER
DG-75 Growth Inhibition Assay IC50=415.698 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=419.185 μM SANGER
KNS-42 Growth Inhibition Assay IC50=425.815 μM SANGER
SH-4 Growth Inhibition Assay IC50=427.565 μM SANGER
L-540 Growth Inhibition Assay IC50=431.031 μM SANGER
NB10 Growth Inhibition Assay IC50=441.234 μM SANGER
ES1 Growth Inhibition Assay IC50=452.753 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=456.711 μM SANGER
MC116 Growth Inhibition Assay IC50=458.116 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=460.005 μM SANGER
RL95-2 Growth Inhibition Assay IC50=460.237 μM SANGER
Raji Growth Inhibition Assay IC50=468.143 μM SANGER
CAS-1 Growth Inhibition Assay IC50=472.073 μM SANGER
Calu-6 Growth Inhibition Assay IC50=475.265 μM SANGER
KG-1 Growth Inhibition Assay IC50=478.44 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=482.232 μM SANGER
ACN Growth Inhibition Assay IC50=493.599 μM SANGER
KM12 Growth Inhibition Assay IC50=496.589 μM SANGER
U2OS Function assay Binding affinity to wild type Smo expressed in U2OS cells by scintillation counting, Kd = 0.0124 μM. 23063522
HCC827 Function assay Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting, Ki = 0.051 μM. 28787156
U2OS Function assay Binding affinity to Smo D473H mutant expressed in U2OS cells by scintillation counting, Kd = 0.116 μM. 23063522
CHO Function assay Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay, IC50 = 0.28 μM. 19091559
Shh-light2 Function assay Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay, IC50 = 0.3 μM. 22268551
Shh Light2 Function assay Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay, EC50 = 0.5 μM. 19309080
C3H10T1/2 Function assay Inhibition of N-terminal SHH activated pathway in mouse C3H10T1/2 cells assessed as SAG-induced cell differentiation by alkaline phosphatase assay, IC50 = 0.6 μM. 21592788
medulloblastoma cells Antiproliferative assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay, EC50 = 1 μM. 17417631
CHO Function assay Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay, IC50 = 1.2 μM. 19091559
MEF Function assay Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli1 transcriptional activity, IC50 = 1.5 μM. 23074541
neural precursor cells Antiproliferative assay Antiproliferative activity against mouse neural precursor cells by colony formation assay, EC50 = 13.44 μM. 17417631
U87 Cytotoxicity assay Cytotoxicity against human U87 cells assessed as viability in presence of beta glucuronidase, IC50 = 15.5 μM. 20116904
A549 Anticancer assay Anticancer activity against human A549 cells by MTS assay, IC50 = 49 μM. 18221872
HEK293 Function assay Inhibition of beta galactosidase in HEK293 cells 17494766
22Rv Function assay Reduction of expression of PTCH mRNA in human 22Rv cells 17494766
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生物活性

產(chǎn)品描述 Cyclopamine (11-deoxojervine)是一種特異性Hedgehog (Hh)信號(hào)通路拮抗劑，作用于Smoothened (Smo)，在TM3Hh12細(xì)胞中IC50為46 nM。
靶點(diǎn)
Smoothened [1]
(TM3Hh12 cells)
46 nM
體外研究(In Vitro)
體外研究活性 Cyclopamine 抑制Hedgehog信號(hào)通路， IC50 為46 nM, 且在[3H]Hh-Ag結(jié)合實(shí)驗(yàn)中，作用于CHO-K1細(xì)胞，抑制人類Smo受體活性，IC50為 280 nM。[1] Cyclopamine作用于表達(dá)Patched (PTCH) mRNA的腸源性腫瘤細(xì)胞，顯著抑制 Hedgehog通路活性，這種作用存在劑量依賴性，且濃度為3 μM時(shí)，抑制腫瘤細(xì)胞生長(zhǎng)，抑制達(dá)75-95%, 但是作用于不表達(dá)PTCH mRNA的結(jié)腸癌細(xì)胞沒有效果，說(shuō)明Cyclopamine 特定作用于Hedgehog 通路，且沒有毒性。[2]通過與Smo直接作用而抑制Hedgehog信號(hào)，Cyclopamine (10 μM) 抑制SMOhigh Cyclopamine-反應(yīng)細(xì)胞系L3.6sl和 Panc 05.04增殖，抑制達(dá) 75-80%,且使凋亡率提高2.5到 3.5倍，但是不影響B(tài)xPC3-SMOlow 細(xì)胞系。[3] Cyclopamine 處理E3LZ10.7細(xì)胞系，顯著降低Snail mRNA，且提供E-鈣粘著蛋白轉(zhuǎn)錄。Cyclopamine處理Hedgehog依賴型 L3.6pl 細(xì)胞，顯著抑制浸潤(rùn)型細(xì)胞, 使轉(zhuǎn)移細(xì)胞降低500多倍，但是對(duì)Hedgehog非依賴性細(xì)胞系Panc-1沒有影響。[4]
激酶實(shí)驗(yàn) 激酶實(shí)驗(yàn)
Gli-Luc實(shí)驗(yàn)測(cè)定Hh 信號(hào)通路末期, 即使用熒光素酶進(jìn)行讀數(shù)，測(cè)定Gli的轉(zhuǎn)錄調(diào)控。Cyclopamine 在DMSO中連續(xù)稀釋用于實(shí)驗(yàn)，然后加到空的實(shí)驗(yàn)板上。TM3Hh12 細(xì)胞(TM3 細(xì)胞含Hh反應(yīng)受體基因結(jié)構(gòu) pTA-8xGli-Luc) 懸浮在含5% FBS 和15 mM Hepes pH 7.3的F12 Ham’s/DMEM (1:1)培養(yǎng)基上, 加到實(shí)驗(yàn)板上，與Cyclopamine在37oC下溫育30分鐘左右。1 nM Hh-Ag 1.5 加到實(shí)驗(yàn)板上，然后在37oC下溫育。48小時(shí)后，在實(shí)驗(yàn)板中加入Bright-Glo或MTS，然后在492 nm處測(cè)定發(fā)光度或吸光度。通過分析反應(yīng)曲線，使用R統(tǒng)計(jì)軟件包測(cè)定IC50值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 SEG1, OE33, KYAE, KYSE180, SNU1, AGS, SNU16, NCI-N-87, HUCCT1, PANC1, PL5, PL6, BXPC3, HS766T, KYSE150, GBD1, DLD1, 和HCT116
濃度 溶于DMSO, 終濃度為3 μM
孵育時(shí)間 4天
方法 在96孔板上，用Cyclopamine 處理細(xì)胞。通過MTS實(shí)驗(yàn)測(cè)定細(xì)胞活力。進(jìn)行CellTiter96比色測(cè)定，進(jìn)行2和4天，然后在490 nm處通過測(cè)定光密度而測(cè)定存活細(xì)胞。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot Snail / E-cadherin / Slug / Vimentin Gli1 / TGF-β1 / CXCR4 NF-κB / Cyclin D1 / MMP2 / MMP9 26859575
Immunofluorescence PCNA / β-catenin Vimentin 28747625
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Cyclopamine 每天按50 mg/kg劑量處理小鼠，持續(xù)22天，消除HUCCT1移植瘤，且沒有明顯副作用。[2] Cyclopamine 按1.2 mg劑量處理Panc 05.04和 L3.6sl驅(qū)動(dòng)的腫瘤7天，前者誘導(dǎo)明顯的腫瘤細(xì)胞凋亡，后者降低腫瘤質(zhì)量，降低達(dá)50-60%，但是作用于BxPC3-SMOlow腫瘤沒有效果。[3] Cyclopamine單獨(dú)處理E3LZ10.7 和L3.6pl移植瘤，顯著抑制腫瘤轉(zhuǎn)移，且和 Gemcitabine聯(lián)用處理，完全廢除轉(zhuǎn)移。[4]
動(dòng)物實(shí)驗(yàn) Animal Models 皮下注射HUCCT1細(xì)胞的無(wú)胸腺裸鼠
Dosages 50 mg/kg/day
Administration 皮下注射處理

化學(xué)信息&溶解度

分子量 411.62 分子式

C27H41NO2
CAS號(hào) 4449-51-8 SDF Download Cyclopamine SDF
Smiles CC1CC2C(C(C3(O2)CCC4C5CC=C6CC(CCC6(C5CC4=C3C)C)O)C)NC1
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

Ethanol : 21 mg/mL (51.01 mM)

DMSO : Insoluble ( ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)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(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)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(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)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，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)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(nèi)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(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 reconstitute the compound for in vivo use in mice?

回答：
One paper dissolved this drug in DMSO, and diluted in saline: Berman DM, et al. Nature, 2003, 425(6960), 846-851. Alternatively, you can try this vehicle: 10% DMSO+30% PEG 300+5% Tween 80+ddH2O for P.O. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG300 and Tween, after they mixed well, dilute with water.

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