VPC 14449

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

VPC 14449 是一种有效的选择性雄激素受体 DNA 结合域 (AR-DBD) 抑制剂，IC50 为 0.34 uM。

VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression; effectively blocks transcriptional activity of full-length and splice variant AR forms at low to sub-micromolar concentrations; reduces tumor volume and abolishes PSA production in LNCaP xenograft model.

Cell Viability Assay Cell Line:LNCaP, C4-2, MR49F, and 22Rv1 cells Concentration:0.01, 0.1, 10, 100 μM Incubation Time:24 hours Result:Suppressed the growth of every tested cell line.Western Blot Analysis Cell Line:LNCaP, C4-2, MR49F, and 22Rv1 cells Concentration:0.01, 0.1, 10, 100 μM Incubation Time:24 hours Result:Inhibited endogenous AR transactivation in LNCaP, C4-2 and MR49F cells stimulated with the synthetic androgen R1881.

Animal Model:Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated Dosage:100 mg/kg Administration:I.p. twice daily for 4 weeks Result:Suppressed LNCaP tumor volume and blocked serum PSA production.

VPC14449

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor (AR)

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1621375-32-3

394.085

C10H10Br2N4OS

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (317.19 mM)

BrC1=C(Br)N=CN1C2=CSC(N3CCOCC3)=N2

4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine

(-20℃)

With Ice Pack

≥ 2 years