| 货号 | 18270-25mg |
| 描述 | PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.1,2 The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.2 The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.1,3 Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.3,4 |
| 别名 | SNX-5422; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Chandarlapaty, S.,Sawai, A.,Ye, Q., et al. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clinical Cancer Research 14(1), 240-248 (2008). 2.Jain, L.,Gardner, E.R.,Venitz, J., et al. Determination of PF-04928473 in human plasma using liquid chromatography with tandem mass spectrometry. Journal of Chromatography.B, Analytical Technologies in the Biomedical and Life Sciences 878(30), 3187-3192 (2010). 3.Okawa, Y.,Hideshima, T.,Steed, P., et al. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood 113(4), 846-855 (2009). 4.Lamoureux, F.,Thomas, C.,Yin, M.J., et al. A novel HSP90 inhibitor delays castrate-resistant prostate cancer without altering serum PSA levels and inhibits osteoclastogenesis. Clinical Cancer Research 17(8), 2301-2313 (2011). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 521.5 |
| 分子式 | C25H30F3N5O4 |
| CAS号 | 908115-27-5 |
| 稳定性 | ≥ 2 years |
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