PF-06747775

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

一种有效的、选择性的、不可逆的 EGFR 突变体，对 EGFR L858R-T790M、Del-T790M、L858R 和 EGFR Del 的 IC50 分别为 12、3、4 和 5 nM。

A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively; displays excellent selectivity over wild-type EGFR (IC50=307 nM), and desirable ADME properties, shows potential for treatment of EGFR T790M mutation in advanced NSCLC.Lung Cancer Phase 2 Clinical.

Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM).Mavelertinib (10 μM) exhibits less than 50% e?ect or inhibition against all nonkinase targets.Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM.

Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg).Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog). Animal Model:Female Nu/Nu mice Dosage:1 mg/kg (Pharmacokinetic Analysis) Administration:P.o. and i.v. administration Result:Oral bioavailability (60%), T1/2 (1.48 h).

PF 06747775 | PF06747775 | PF 6747775

Angiogenesis

EGFR

EGFR

Cancer

Lung Cancer

1776112-90-3

415.433

C18H22FN9O2

>98% (HPLC)

In Vitro:?DMSO : 47.5 mg/mL (114.34 mM)

C=CC(N[C@@H]1CN(C2=NC(NC3=CN(C)N=C3OC)=C4N=CN(C)C4=N2)C[C@H]1F)=O

N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidin-3-yl)acrylamide

(-20℃)

With Ice Pack

≥ 2 years