AZ-23是一种 ATP-竞争性的,口服具有活性的Trk激酶 A/B/C抑制剂,IC50值分别为2 nM (TrkA),8 nM (TrkB),24 nM (FGFR1),52 nM (FLT3),55 nM (Ret),84 nM (MuSk),99 nM (Lck)。
产品描述
AZ-23 is an inhibitor of ATP-competitive and Trk kinase A/B/C. For TrkA, TrkB, FGFR1, Flt3, Ret, MuSk, Lck, the IC50s values are 2 nM, 8 nM, 24 nM, 52 nM, 55 nM, 84 nM, 99 nM, respectively.
体外活性
AZ-23 potently and selectivity inhibits Trk phosphorylation in cells. AZ-23 potently inhibits Trk-mediated survival (EC50 of 2 nM) and it also Inhibits Trk-Dependent Survival in MCF10ATrkA-Δ and TF-1 Cell Lines[1].
体内活性
AZ-23 shows in vivo TrkA kinase inhibition and efficacy in mice following oral administration in a TrkA-driven allograft model. And it significant tumor growth inhibition in a Trk-expressing xenograft model of neuroblastoma[1].
Cas No.
915720-21-7
分子式
C17H19ClFN7O
分子量
391.83
别名
AZ23;AZ 23
储存和溶解度
DMSO:125 mg/mL (319.02 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years