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• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *