Vismodegib (GDC-0449)

    
99%

Vismodegib (GDC-0449)

源叶(MedMol)
S81056 一键复制产品信息
879085-55-9
C19H14Cl2N2O3S
421.31
GDC-0449;GDC 0449;GDC0449;2-氯-N-[4-氯-3-(2-吡啶基)苯基]-4-(甲磺酰基)苯甲酰胺
货号 规格 价格 上海 北京 武汉 南京 购买数量
S81056-5mg 99% ¥50.00 7 - - -
S81056-10mg 99% ¥69.00 8 - - -
S81056-50mg 99% ¥218.00 3 - - -
S81056-100mg 99% ¥340.00 货期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

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

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
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参考文献

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