| 货号 | 17810-1mg |
| 描述 | Inhibitor of apoptosis proteins (IAPs), which block various signaling pathways leading to apoptotic cell death, are commonly over-expressed in cancer cells.1 GDC-0152 is a potent inhibitor of specific IAPs that binds baculoviral IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively).2 GDC-0152 induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.2,3 It is orally bioavailable and suppresses tumor growth in breast cancer xenografts in mice.2 GDC-0152 also induces NF-κB transcriptional activity, resulting in the expression of several cytokines, including TNF-α.4 In dogs and rats, but not humans, this leads to a pronounced inflammatory response.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Goyal, L. Cell death inhibition:Keeping caspases in check. Cell 104, 805-808 (2001). 2.Flygare, J.A.,Beresini, M.,Budha, N., et al. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). Journal of Medicinal Chemistry 55(9), 4101-4113 (2012). 3.Hu, R.,Li, J.,Liu, Z., et al. GDC-0152 induces apoptosis through down-regulation of IAPs in human leukemia cells and inhibition of PI3K/Akt signaling pathway. Tumour Biology 36(2), 577-584 (2015). 4.Erickson, R.I.,Tarrant, J.,Cain, G., et al. Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-α pharmacology. Toxicological Sciences 131(1), 247-258 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 498.6 |
| 分子式 | C25H34N6O3S |
| CAS号 | 873652-48-3 |
| 稳定性 | ≥ 2 years |
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