| 产品描述： | Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively |
| 靶点： |
IC50: 3 nM (hedgehog), 3.0 μM (P-gp), 1.4 μM (ABCG2);Hedgehog/Smoothened; ABC; Autophagy |
| 体内研究： |
Vismodegib is a novel small molecule HPI, often used for clinical trials. Vismodegib (0.3 to 75 mg/kg, p.o.) is highly efficacious in medulloblastoma allograft tumors. Vismodegib (> 46 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts |
| 参考文献： |
1. Scales SJ, et al. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol Sci. 2009, 30(6), 303-312. 2. Zhang Y, et al. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia. 2009, 11(1), 96-101. 3. Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in NSC 119875-resistant lung cancer cells. Anticancer Res. 2012, 32(1), 89-94. 4. Wong H, et al. Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation. Clin Cancer Res. 2011, 17(14), 4682-4692. 5. Elhenawy AA, et al. Possible antifibrotic effect of GDC-0449 (Vismodegib), a hedgehog-pathway inhibitor, in mice model of Schistosoma-induced liver fibrosis. Parasitol Int. 2017 Oct;66(5):545-554. 6. Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246. |
| 溶解性： |
DMSO : 50 mg/mL (118.68 mM; Need ultrasonic) Ethanol : 3.33 mg/mL (7.90 mM; ultrasonic and warming and heat to 60°C) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.374 ml |
11.868 ml |
23.735 ml |
| 5 mM |
0.475 ml |
2.374 ml |
4.747 ml |
| 10 mM |
0.237 ml |
1.187 ml |
2.374 ml |
| 50 mM |
0.047 ml |
0.237 ml |
0.475 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京