AMG-208

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AMG-208 是一种有效的小分子 c-Met 抑制剂，针对 wt MET 激酶的 IC50 为 5.2 nM，还抑制 VEGFR2，IC50 为 112 nM。

AMG-208 is a potent, small-molecule c-Met inhibitor with IC50 of 5.2 nM against wt MET kinase, also inhibits VEGFR2 with IC50 of 112 nM; inhibits HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM, suppresses proliferation and induces apoptosis in human tumor xenograft models.Prostate Cancer Phase 2 Clinical(In Vitro):AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM.Pre-incubation of AMG-208 (compound 1) with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation.(In Vivo):In male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour.

AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. Pre-incubation of AMG-208 (compound 1) with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation.

In male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour.

AMG208 | AMG 208

Angiogenesis

c-Met/HGFR

c-Met

Cancer

Prostate Cancer

1002304-34-8

383.4027

C22H17N5O2

>98% (HPLC)

DMSO: < 1 mg/mL

COC1=CC=C2C(OCC3=NN=C4C=CC(C5=CC=CC=C5)=NN43)=CC=NC2=C1

Quinoline, 7-methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]-

(-20℃)

With Ice Pack

≥ 2 years