| 货号 | 13613-50mg |
| 描述 | Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.1 GDC-0449 is a potent antagonist of SMO that acts in a biphasic manner, with apparent high affinity (Ki = 1.3 nM) and low affinity (Ki = 2.3 µM) binding.2 It suppresses Gli-mediated transcription in Calu-6 tumors with an IC50 value of 13 nM and prevents hedgehog-dependent medulloblastoma allograft growth in mice.3 GDC-0449 less potently inhibits the ATP-binding cassette (ABC) proteins ABCG2 and ABCB1 (IC50 = 1.4 and 3.0 µM, respectively), which may ameliorate drug resistance.4 This compound has potential applications in several forms of cancer, including basal cell carcinoma.5,6 |
| 别名 | Vismodegib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ruiz-Gómez, A.,Molnar, C.,Holguín, H., et al. The cell biology of Smo signalling and its relationships with GPCRs. Biochimica et Biophysica Acta 1768(4), 901-912 (2007). 2.Rominger, C.M.,Bee, W.L.T.,Copeland, R.A., et al. Evidence for allosteric interactions of antagonist binding to the smoothened receptor. Journal of Pharmacology and Experimental Therapeutics 329(3), 995-1005 (2009). 3.Robarge, K.D.,Brunton, S.A.,Castanedo, G.M., et al. GDC-0449 - A potent inhibitor of the hedgehog pathway. Bioorganic & Medicinal Chemistry Letters 19(19), 5576-5581 (2009). 4.Zhang, Y.,Laterra, J., and Pomper, M.G. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia 11(1), 96-101 (2009). 5.Scales, S.J., and de Sauvage, F.J. Mechanisms of hedgehog pathway activation in cancer and implications for therapy. Trends in Pharamacological Sciences 30(6), 303-312 (2009). 6.Lyseng-Williamson, K.A., and Keating, G.M. Vismodegib. A guide to its use in locally advanced or metastatic basal cell carcinoma. Am.J.Clin.Dermatol. 14(1), 61-64 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 421.3 |
| 分子式 | C19H14Cl2N2O3S |
| CAS号 | 879085-55-9 |
| 稳定性 | ≥ 2 years |
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