GDC046

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

GDC046 是一种有效的先导类似物，具有良好的激酶选择性、理化特性和药代动力学特征。

GDC046, a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.

In cell-based assays, GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) while displaying less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM) and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM).

In mice, GDC-046 exhibits relatively high clearance (65 mL/min/kg) when dosed intravenously (i.v. 1 mg/kg) and exhibits modest oral exposure (AUC=2.6 μM·h at p.o. 5 mg/kg).

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Others

Other Targets

Others

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1258292-64-6

350.2

C16H13Cl2N3O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (178.47 mM)

Clc1cccc(Cl)c1C(=O)Nc1ccnc(NC(=O)C2CC2)c1

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(-20℃)

With Ice Pack

≥ 2 years