A939572

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

A939572 是硬脂酰辅酶 A 去饱和酶 1 (SCD1) 抑制剂，mSCD1 的 IC50 值 < 4 nM，hSCD1 的 IC50 值 < 37 nM。

A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.(In Vitro):A939572 exhibits robust in vivo activity with dose-dependent desaturation index lowering effects. A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC50s of 65 nM, 50 nM, 65 nM, and 6 nM, respectively). In A939572 (SCDi) treated Caki1 and A498 cells, all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control, and this elevated expression can be blocked with the addition of OA-BSA.(In Vivo):Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg, p.o.) and Tem individually or in combination over the course of four weeks, and tumor volume (mm3) is recorded. A939572 and Tem monotherapy generate similar growth responses with approximately 20-30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment. The combination group yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment.

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Metabolic Enzyme/Protease

Dehydrogenase

mSCD1/hSCD1

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1032229-33-6

387.85

C20H22ClN3O3

>98% (HPLC)

DMSO:56 mg/mL?(144.38 mM)

CNC(=O)c1cccc(NC(=O)N2CCC(CC2)Oc2ccccc2Cl)c1

(Z)-4-(2-chlorophenoxy)-N-(3-((Z)-hydroxy(methylimino)methyl)phenyl)piperidine-1-carbimidic acid

(-20℃)

With Ice Pack

≥ 2 years