Vismodegib
产品说明书
 |
同义名 : | GDC-0449 |
| CAS号 : | 879085-55-9 | |
| 货号 : | A603143 | |
| 分子式 : | C19H14Cl2N2O3S | |
| 纯度 : | 98% | |
| 分子量 : | 421.297 | |
| MDL号 : | MFCD12407408 | |
| 存储条件： |
Pure form Sealed in dry,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 50 mg/mL(118.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 3 mg/mL(7.12 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
|
| 动物实验配方： |
5% DMSO+40% PEG 300+5% Tween 80+50% water 12.5 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The Hedgehog (HH) signaling pathway is closely linked to developmental processes, organ patterning, tissue and stem cell maintenance, cell differentiation processes, cell proliferation, regenerative responses after injury and cancer formation[6]. Vismodegib (GDC-0449) is a potent inhibitor of two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, with IC50 values of 1.4 and 3.0 µM, respectively. Additionally, vismodegib can also mildly inhibit ABCC1/MRP1 [7]. In vitro, vismodegib can inhibited cell viability and induce apoptosis in pancreatic cancer cell lines (AsPC-1, PANC-1 and MIA PaCa-2) at 72 hours with IC50 less than 10 μM. Vismodegib-induced apoptosis in cancer cell lines showed increased Fas expression and decreased expression of PDGFRa[8]. After exposed to 50 μM vismodegib for 2 days, survival fraction of HCC and H1339 cells reduced to 60% and 50%, respectively. Ca2+ imaging showed that vismodegib increased [Ca2+](cyto) and reduced endoplasmatic [Ca2+](ER)[1]. When the mouse model of nonalcoholic steatohepatitis was treated with vismodegib (25 mg/kg), TRAIL-mediated liver injury was significantly suppressed and serum ALT and hepatic TUNEL-positive cells were reduced[9]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 23132-87 | Growth Inhibition Assay | IC50=4.40147 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=25.6331 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=44.8023 μM | SANGER | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03498521 | Cancer of Unknown Primary Site | Phase 2 | Recruiting | April 16, 2022 | - |
| NCT03297606 | Lymphoma, Non-Hodgkin ... 展开 >> Multiple Myeloma Advanced Solid Tumors 收起 << | Phase 2 | Recruiting | September 2021 | Canada, British Columbia ... 展开 >> BCCA - Vancouver Cancer Centre Recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Daniel John Renouf 604 877-6000 ext 672357 Canada, Ontario London Regional Cancer Program Recruiting London, Ontario, Canada, N6A 5W9 Contact: Stephen Welch 519 685-8640 Ottawa Hospital Research Institute Recruiting Ottawa, Ontario, Canada, K1H 8L6 Contact: John Hilton 613 737-7700 ext 70179 University Health Network Recruiting Toronto, Ontario, Canada, M5G 2M9 Contact: Lillian Siu 416 946-2911 Canada, Quebec The Jewish General Hospital Recruiting Montreal, Quebec, Canada, H3T 1E2 Contact: Cristiano Ferrario 514 398-8307 收起 << |
| NCT02788201 | Urothelial Carcinoma ... 展开 >> Bladder Cancer Urinary Bladder Neoplasms 收起 << | Phase 2 | Recruiting | July 1, 2020 | United States, Maryland ... 展开 >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office 888-624-1937 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.87mL 2.37mL 1.19mL |
23.74mL 4.75mL 2.37mL |
| 参考文献 |
|---|