Cyclopamine
别名: 11-deoxojervine 中文名称：环巴胺
Cyclopamine (11-deoxojervine)是一种特异性Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，在TM3Hh12细胞中IC50为46 nM。
Cyclopamine Chemical Structure
CAS: 4449-51-8
客户使用Selleck的Cyclopamine发表文献132篇
产品质控
批次：
纯度：
99.98%
99.98
Cyclopamine相关产品
相关信号通路图
Hedgehog/Smoothened抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Cyclopamine (11-deoxojervine)是一种特异性Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，在TM3Hh12细胞中IC50为46 nM。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Cyclopamine 抑制Hedgehog信号通路， IC50 为46 nM, 且在[3H]Hh-Ag结合实验中，作用于CHO-K1细胞，抑制人类Smo受体活性，IC50为 280 nM。[1] Cyclopamine作用于表达Patched (PTCH) mRNA的肠源性肿瘤细胞，显著抑制 Hedgehog通路活性，这种作用存在剂量依赖性，且浓度为3 μM时，抑制肿瘤细胞生长，抑制达75-95%, 但是作用于不表达PTCH mRNA的结肠癌细胞没有效果，说明Cyclopamine 特定作用于Hedgehog 通路，且没有毒性。[2]通过与Smo直接作用而抑制Hedgehog信号，Cyclopamine (10 μM) 抑制SMOhigh Cyclopamine-反应细胞系L3.6sl和 Panc 05.04增殖，抑制达 75-80%,且使凋亡率提高2.5到 3.5倍，但是不影响BxPC3-SMOlow 细胞系。[3] Cyclopamine 处理E3LZ10.7细胞系，显著降低Snail mRNA，且提供E-钙粘着蛋白转录。Cyclopamine处理Hedgehog依赖型 L3.6pl 细胞，显著抑制浸润型细胞, 使转移细胞降低500多倍，但是对Hedgehog非依赖性细胞系Panc-1没有影响。[4] | |||
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| 激酶实验 | 激酶实验 | |||
| Gli-Luc实验测定Hh 信号通路末期, 即使用荧光素酶进行读数，测定Gli的转录调控。Cyclopamine 在DMSO中连续稀释用于实验，然后加到空的实验板上。TM3Hh12 细胞(TM3 细胞含Hh反应受体基因结构 pTA-8xGli-Luc) 悬浮在含5% FBS 和15 mM Hepes pH 7.3的F12 Ham’s/DMEM (1:1)培养基上, 加到实验板上，与Cyclopamine在37oC下温育30分钟左右。1 nM Hh-Ag 1.5 加到实验板上，然后在37oC下温育。48小时后，在实验板中加入Bright-Glo或MTS，然后在492 nm处测定发光度或吸光度。通过分析反应曲线，使用R统计软件包测定IC50值。 | ||||
| 细胞实验 | 细胞系 | SEG1, OE33, KYAE, KYSE180, SNU1, AGS, SNU16, NCI-N-87, HUCCT1, PANC1, PL5, PL6, BXPC3, HS766T, KYSE150, GBD1, DLD1, 和HCT116 | ||
| 浓度 | 溶于DMSO, 终浓度为3 μM | |||
| 孵育时间 | 4天 | |||
| 方法 | 在96孔板上，用Cyclopamine 处理细胞。通过MTS实验测定细胞活力。进行CellTiter96比色测定，进行2和4天，然后在490 nm处通过测定光密度而测定存活细胞。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Snail / E-cadherin / Slug / Vimentin Gli1 / TGF-β1 / CXCR4 NF-κB / Cyclin D1 / MMP2 / MMP9 |
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26859575 | |
| Immunofluorescence | PCNA / β-catenin Vimentin |
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28747625 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Cyclopamine 每天按50 mg/kg剂量处理小鼠，持续22天，消除HUCCT1移植瘤，且没有明显副作用。[2] Cyclopamine 按1.2 mg剂量处理Panc 05.04和 L3.6sl驱动的肿瘤7天，前者诱导明显的肿瘤细胞凋亡，后者降低肿瘤质量，降低达50-60%，但是作用于BxPC3-SMOlow肿瘤没有效果。[3] Cyclopamine单独处理E3LZ10.7 和L3.6pl移植瘤，显著抑制肿瘤转移，且和 Gemcitabine联用处理，完全废除转移。[4] | |
|---|---|---|
| 动物实验 | Animal Models | 皮下注射HUCCT1细胞的无胸腺裸鼠 |
| Dosages | 50 mg/kg/day | |
| Administration | 皮下注射处理 | |
化学信息&溶解度
| 分子量 | 411.62 | 分子式 | C27H41NO2 |
| CAS号 | 4449-51-8 | SDF | Download Cyclopamine SDF |
| Smiles | CC1CC2C(C(C3(O2)CCC4C5CC=C6CC(CCC6(C5CC4=C3C)C)O)C)NC1 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
Ethanol : 2 mg/mL DMSO : Insoluble ( DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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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