CO-1686

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and L858R mutant kinases demonstrates the highest degree of inhibition at 0.1 uM; orally bioavailable.Lung Cancer Withdrawn(In Vitro):Rociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets.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.(In Vivo):Rociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice.

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Rociletinib | AVL-301 | CNX-419

Angiogenesis

EGFR

EGFR(L858R/T790M)|EGFR(wt)

Cancer

Lung Cancer

1374640-70-6

555.5515

C27H28F3N7O3

>98% (HPLC)

DMSO: ≥ 43 mg/mL

C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O

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

(-20℃)

With Ice Pack

≥ 2 years