Lifirafenib

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

在生化测定中，Lifirafenib 是 RAF 家族激酶和 EGFR 的有效抑制剂，对重组 BRAFV600E 激酶结构域、EGFR 和 EGFR T790M/L858R 突变体的 IC50 分别为 23、29 和 495 nM。

Lifirafenib is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively.

Lifirafenib (BGB-283) potently inhibits BRafV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRafV600E and EGFR mutation/amplification. In BRafV600E colorectal cancer cell lines, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation.

Lifirafenib (BGB-283) treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRafV600E mutation.

Beigene-283 | BGB-283

Angiogenesis

EGFR

B-Raf (V600E)|EGFR|EGFR (L858R/T790M)

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1446090-79-4

478.42

C25H17F3N4O3

>98% (HPLC)

DMSO:100 mg/mL (209.02 mM)

O=C1Nc2nccc(Oc(cc3)cc(C45)c3OC4C5c3nc(ccc(C(F)(F)F)c4)c4[nH]3)c2CC1

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(-20℃)

With Ice Pack

≥ 2 years