CAS NO: | 1688673-09-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Pamufetinib (TAS-115) mesylate is a potentVEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, withIC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. | ||||||||||||||||
IC50& Target | IC50: 30 nM (rVEGFR2), 32 nM (rMET)[1] | ||||||||||||||||
体外研究 (In Vitro) | Pamufetinib mesylate powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI50=0.032-0.362 μM) as a MET-targeted inhibitor. Pamufetinib mesylate has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors[1]. Crizotinib and Pamufetinib mesylate inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells[2]. | ||||||||||||||||
体内研究 (In Vivo) | Pamufetinib mesylate completely suppresses the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of Pamufetinib mesylate. Pamufetinib mesylate induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 614.66 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C28H27FN4O7S2 | ||||||||||||||||
CAS 号 | 1688673-09-7 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 75 mg/mL(122.02 mM;Need ultrasonic) 配制储备液
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