CO-1686 hydrobromide

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、高选择性的、不可逆的突变型 EGFR 抑制剂，对 EGFR L858R/T790M 的 Ki 值为 21.5 nM。

A potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M; shows 22-fold selective over WT EGFR; EGFR del19, T790M, L858R/T790M and L858R mutant kinases demonstrates the highest degree of inhibition at 0.1 uM; orally bioavailable.Breast Cancer Phase 2 Clinical.

Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition.

Rociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice.

Rociletinib hydrobromide | AVL-301 hydrobromide | CNX-419 hydrobromide

Angiogenesis

EGFR

EGFR

Cancer

Breast Cancer

1446700-26-0

636.4634

C27H29BrF3N7O3

>98% (HPLC)

DMSO: ≥ 59 mg/mL

CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC.Br

2-Propenamide, N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-, hydrobromide (1:1)

(-20℃)

With Ice Pack

≥ 2 years