货号	规格	价格	上海	北京	武汉	南京
S81006-5mg	≥98%	￥500.00 S81006-5mg ￥500.00 现货	5 5	-	-	-
S81006-25mg	≥98%	￥870.00 S81006-25mg ￥870.00 现货	6 6	-	-	-
S81006-100mg	≥98%	￥1900.00 S81006-100mg ￥1900.00 现货	8 8	-	-	-

产品介绍

Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).

产品描述：

Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).

靶点：

IC50: 47 nM (CYP17);P450; AndrogenReceptor

体内研究：

Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of Galeterone (TOK-001) twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p= 0.0001). Galeterone (TOK-001) treatment also significantly reduces the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with Galeterone (TOK-001) compared to animals treated with control, and castration (p<0.05)

参考文献：

1. Bruno RD, et al. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.Steroid 2. DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001.Nature. 2012 Jan 22;482(7383):116-9. 3. Soifer HS, et al. Direct regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cells.J Biol Chem. 2012 Feb 3;287(6):3777-87. Epub 2011 Dec 15.

溶解性：

DMSO : 25 mg/mL (64.34 mM; Need ultrasonic)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.574 ml	12.868 ml	25.736 ml
5 mM	0.515 ml	2.574 ml	5.147 ml
10 mM	0.257 ml	1.287 ml	2.574 ml
50 mM	0.051 ml	0.257 ml	0.515 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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