Rezivertinib

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

Rezivertinib (BPI-7711) 是一种口服有效，高选择性和不可逆的第三代 EGFR 酪氨酸激酶抑制剂 (TKI)。Rezivertinib 对常见的激活 EGFR 和抗性T790M 突变具有高效力。Rezivertinib 具有出色的透过中枢神经系统 (CNS) 能力，并具有抗肿瘤活性。

Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.

Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT).

Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression.Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model. Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days).

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Angiogenesis

EGFR

EGFR

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1835667-12-3

486.57

C27H30N6O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (256.90 mM; 超声助溶 )

O=C(C=C)NC1=CC(NC=2N=CC=C(N2)C3=CN(C=4C=CC=CC34)C)=C(OC)C=C1OCCN(C)C

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(-20℃)

With Ice Pack

≥ 2 years