Varlitinib

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

Varlitinib 是一种选择性有效的 ErbB1(EGFR) 和 ErbB2(HER2) 抑制剂，IC50 分别为 7 nM 和 2 nM。

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM respectively. Phase 2.

In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) potently inhibits substrate phosphorylation. Varlitinib is shown to be highly selective for EGFR/ErbB-2, and does not show any significant activity when screened against a panel of 104 kinases.

Varlitinib treatment potently inhibits tumor growth with complete tumor regression observed at dosing of 100 mg/kg twice a day. After five days of Varlitinib treatment, phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal, 4EBP1, Cdk-2, Cdc-2 and retinoblastoma are strongly inhibited. Varlitinib treatment results in a significant reduction in survivin and a concomittant increase in Caspase 3 cleavage products. In murine xenograft models, Varlitinib (ARRY-334543) demonstrates significant dose-related (25, 50, 100 mg/kg) tumor growth inhibition in A431-derived tumors when administered orally, twice a day, for 21 days.

ASLAN001 | ARRY-334543

Angiogenesis

EGFR

EGFR/ErbB1| HER2/ErbB2

Cancer

Biliary Cancer

845272-21-1

466.94

C22H19ClN6O2S

>98% (HPLC)

DMSO:6 mg/mL (12.84 mM);Ethanol:<1 mg/mL;Water:<1 mg/mL

C[C@@H]1COC(NC2=CC3=C(C=C2)N=CN=C3NC2=CC(Cl)=C(OCC3=NC=CS3)C=C2)=N1

(R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-45-dihydrooxazol-2-yl)quinazoline-46-diamine.

(-20℃)

With Ice Pack

≥ 2 years