LDE225 (phosphate)
货号：
16263-1mg 基本售价：
490.0 元 规格：
1 mg
产品信息
概述| 货号 | 16263-1mg |
| 描述 | Hedgehog (Hh) proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of the GPCR-like receptor, Smoothened (SMO).1 In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the Gli family. Overactivation of this pathway contributes to certain cancers.2 LDE225 is an Hh signaling pathway inhibitor that acts by antagonizing SMO (IC50s = 1.3 and 2.5 nM for mouse and human, respectively).3 A dose of 20 mg/kg/day LDE225 has been shown to penetrate the blood brain barrier, inhibit Gli1 mRNA expression, and prevent tumor growth in a medulloblastoma allograft mouse model.3 This compound has been investigated in phase II clinical trials for potential treatment of several Hh pathway activated cancers. |
| 别名 | Erismodegib;NVP-LDE225;Sonidegib; |
性能| 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.Rubin, L.L. and de Sauvage, F.J. Targeting the Hedgehog pathway in cancer. Nature Reviews.Drug Discovery 5(12), 1026-1033 (2006).
3.Pan, S.,Wu, X.,Jiang, J., et al. Discovery of NVP-LDE225, a potent and selective smoothened antagonist. ACS Med.Chem.Lett. 1(3), 130-134 (2010).
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| 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 | 681.5 |
| 分子式 | C26H26F3N3O3 • 2H3PO4 |
| CAS号 | 1218778-77-8 |
| 稳定性 | ≥ 2 years |
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