Bavdegalutamide ARV-110|cas:2222112-77-6|西域试剂

Bavdegalutamide ARV-110,98.12%

产品编号：Bellancom-138641| CAS NO：2222112-77-6| 分子式：C₄₁H₄₃ClFN₉O₆| 分子量：812.29

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-138641	￥1460.00	杭州北京（现货）
Bellancom-138641	￥2270.00	杭州北京（现货）
Bellancom-138641	￥4470.00	杭州北京（现货）
Bellancom-138641	￥6670.00	杭州北京（现货）
Bellancom-138641	￥9970.00	杭州北京（现货）

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Bavdegalutamide ARV-110

产品介绍

Bavdegalutamide (ARV-110) 是一种具有口服活性的，特异性的雄激素受体 (AR) PROTAC 类降解剂。Bavdegalutamide 能促进 AR 的泛素化和降解，可用于前列腺癌的研究。

生物活性

Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer.

体外研究

Bavdegalutamide completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC₅₀) < 1 nM.
Bavdegalutamide (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner.
Bavdegalutamide (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner.
Bavdegalutamide (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations.
Bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells.

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

体内研究

Bavdegalutamide (oral gavage; 1 mg/kg; QD) exhibits a greater than 90% AR degradation in vivo. In LNCaP, VCaP and prostate cancer patient derived xenograft (PDX) models, Bavdegalutamide also exhibits significant inhibition of tumor growth and AR signaling.
Bavdegalutamide (oral gavage; 3 or 10 mpk; 30 days) demonstrates in vivo efficacy and reduction of AR-target gene expression in a long term, castrate, enzalutamide-resistant VCaP tumor model. The TGI are 70% and 60% for 3 mpk and 10 mpk dosage. Respectively.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 26.67 mg/mL (32.83 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2311 mL	6.1554 mL	12.3109 mL
5 mM	0.2462 mL	1.2311 mL	2.4622 mL
10 mM	0.1231 mL	0.6155 mL	1.2311 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)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.79 mg/mL (0.97 mM); Clear solution

此方案可获得 ≥ 0.79 mg/mL (0.97 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 7.9 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液