LY2801653,抑制Met (c-Met)酪氨酸激酶

LY2801653 (订货以英文为准)

编号:L127298
CAS号:1206799-15-6
分子式:C30H22F2N6O3
分子量:552.53
货号 品牌 包装 目录价 您的价格 库存 数量 购买
L127298-5mg 阿拉丁 5mg ¥440.90
L127298-10mg 阿拉丁 10mg ¥771.90
L127298-50mg 阿拉丁 50mg ¥3097.90
L127298-100mg 阿拉丁 100mg ¥4738.90
L127298-25mg 阿拉丁 25mg ¥1639.90
产品名称 LY2801653
中文名称 LY2801653,抑制Met (c-Met)酪氨酸激酶
CAS号 1206799-15-6
分子式(M.F.) C30H22F2N6O3
分子量(M.W.) 552.53
储存条件 -20°C储存
溶解性DMSO
存贮条件储存温度-20°C
生化机理Description:IC50 Value: 2 nM(Ki value) [1]LY2801653 is a potent, orally bioavailable, small-molecule inhibitorLY2801653 targeting MET kinase.in vitro: LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (K(i)) of 2 nM, a pharmacodynamic residence time (K(off)) of 0.00132 min(-1) and t(1/2) of 525 min [1]. LY2801653 was found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and against the serine/threonine kinases MKNK1/2.in vivo: LY2801653 demonstrated in vitro effects on MET pathway-dependent cell scattering and cell proliferation; in vivo anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects [1].Clinical trial: LY2801653 is currently in phase 1 clinical testing in patients with advanced cancer (trial I3O-MC-JSBA, NCT01285037).
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