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). |
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
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 |
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