ARD-2128|cas:2222111-87-5|西域试剂

ARD-2128,99.40%

产品编号：Bellancom-132292| CAS NO：2222111-87-5| 分子式：C₄₅H₅₀ClN₇O₆| 分子量：820.37

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-132292		￥7000.00	杭州北京（现货）
Bellancom-132292		￥11500.00	杭州北京（现货）

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ARD-2128

产品介绍

ARD-2128 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂。ARD-2128 可有效降低 AR 蛋白并抑制肿瘤组织中 AR 调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。ARD-2128 作用在前列腺癌的研究上。

生物活性

ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.

体外研究

ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC₅₀ values of 4 nM and 5 nM, respectively.
ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	VCaP cell
Concentration:	1, 10, 100, and 1000 nM
Incubation Time:	24 hours
Result:	Reduces the AR protein level and achieves the AR degradation.

体内研究
(In Vivo)

ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours.
ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice.
ARD-2128 (5mg/kg; p.o.) treatment shows the C_max, AUC_0-t and t_1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice
Dosage:	20 mg/kg
Administration:	Oral
Result:	Reducing the level of AR protein in mice after 24 hours.

Animal Model:	SCID mice
Dosage:	10, 20, and 40 mg/kg
Administration:	P.o.; daily for 21 days
Result:	Inhibits tumor growth by 46, 69, and 63%, respectively.

Animal Model:	Male ICR Mice
Dosage:	5 mg/kg
Administration:	P.o. (Pharmacokinetic Analysis)
Result:	The C_max, AUC_0-t and t_1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice
Dosage:	20 mg/kg
Administration:	Oral
Result:	Reducing the level of AR protein in mice after 24 hours.

Animal Model:	SCID mice
Dosage:	10, 20, and 40 mg/kg
Administration:	P.o.; daily for 21 days
Result:	Inhibits tumor growth by 46, 69, and 63%, respectively.

Animal Model:	Male ICR Mice
Dosage:	5 mg/kg
Administration:	P.o. (Pharmacokinetic Analysis)
Result:	The C_max, AUC_0-t and t_1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice
Dosage:	20 mg/kg
Administration:	Oral
Result:	Reducing the level of AR protein in mice after 24 hours.

Animal Model:	SCID mice
Dosage:	10, 20, and 40 mg/kg
Administration:	P.o.; daily for 21 days
Result:	Inhibits tumor growth by 46, 69, and 63%, respectively.

Animal Model:	Male ICR Mice
Dosage:	5 mg/kg
Administration:	P.o. (Pharmacokinetic Analysis)
Result:	The C_max, AUC_0-t and t_1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (121.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2190 mL	6.0948 mL	12.1896 mL
5 mM	0.2438 mL	1.2190 mL	2.4379 mL
10 mM	0.1219 mL	0.6095 mL	1.2190 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

参考文献