Androgen receptor-IN-2

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CAS NO:

2416716-62-4

Androgen receptor-IN-2 是一种有效的、具有口服活性的androgen receptor抑制剂。Androgen receptor-IN-2 对前列腺癌具有抗肿瘤活性。

生物活性

Androgen receptor-IN-2 is a potent and orally activeandrogen receptorinhibitor. Androgen receptor-IN-2 has antitumor activity against prostatecancer^[1].

IC₅₀& Target

Androgen receptor^[1]

体外研究
(In Vitro)

Androgen receptor-IN-2 (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC₅₀of 535 nM^[1].
Androgen receptor-IN-2 inhibits cell proliferation in LNCaP and LNCaP95 cells (IC₅₀: 0.44 μM, 3.78 μM respectively)^[1].
Androgen receptor-IN-2 shows a metabolic stability in liver microsome with a t_1/2of more than 120 min, and in hepatocytes with a t_1/2of more than 360 min^[1].

体内研究
(In Vivo)

Androgen receptor-IN-2 (compound A109) (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors^[1].
Androgen receptor-IN-2 (5 mg/kg, p.o., single dose, in male CD-1 mice) shows a t_1/2of 8.1 h, C_maxof 2673.3 ng/mL, F (%) of 33.6^[1].

Animal Model:	LNCaP Xenografts Model^[1]
Dosage:	60 mg/kg
Administration:	Oral administration (p.o.)
Result:	Inhibited tumor growth no obvious drug related toxicity (bodyweight change).

分子量

535.44

性状

Solid

Formula

C₂₄H₂₄Cl₂N₄O₄S

CAS 号

2416716-62-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL(93.38 mM;Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.8676 mL	9.3381 mL	18.6762 mL
5 mM	0.3735 mL	1.8676 mL	3.7352 mL
10 mM	0.1868 mL	0.9338 mL	1.8676 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。