ASTX029

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

ASTX029 是一种选择性、口服生物可利用的细胞外信号调节激酶 1 和 2 (ERK 1/2) 抑制剂，具有潜在的抗肿瘤活性。

ASTX029 is a selective and orally bioavailable extracellular signal-regulated kinases 1 and 2 (ERK 1/2) inhibitor, with potential antineoplastic activity.

Western Blot Analysis Cell Line:A375 and HCT116 cells Concentration:1 nM-100 nM Incubation Time:2 h Result:Decreased pRSK and pERK.Apoptosis Analysis Cell Line:A375 and HCT116 cells Concentration:0-100 nM Incubation Time:0-72 h Result:Arrested cell in the G1-phase.Increased cleaved PARP and Bim protein level.

Animal Model:Colo205, A375, Calu-6, HCC44, HCT116 or MA-MEL-28 xenografts tumor-bearing mice Dosage:75 mg/kg Administration:p.o., once daily Result:Inhibited tumor growth in various tumor models.

ASTX-029

MAPK/ERK Signaling

ERK

ERK1/2

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2095719-92-7

584.04

C29H31ClFN5O5

>98% (HPLC)

DMSO：98 mg/mL (167.8 mM); Ethanol:48 mg/mL (82.2 mM)

COC1=CC(F)=CC(=C1)[C@@H](CO)NC(=O)[C@@H](C)N1CC2=CC=C(C=C2C1=O)C1=NC(NC2CCOCC2)=NC=C1Cl

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(-20℃)

With Ice Pack

≥ 2 years