H3B-5942|cas:2052128-15-9|西域试剂

H3B-5942,98.0%

产品编号：Bellancom-112611| CAS NO：2052128-15-9| 分子式：C₃₁H₃₄N₄O₂| 分子量：494.63

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-112611	￥650.00	杭州北京（现货）
Bellancom-112611	￥1900.00	杭州北京（现货）
Bellancom-112611	￥3000.00	杭州北京（现货）
Bellancom-112611	￥5800.00	杭州北京（现货）
Bellancom-112611	￥9900.00	杭州北京（现货）

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H3B-5942

产品介绍

H3B-5942 是一种选择性、不可逆、可口服的 estrogen receptor 共价拮抗剂，能够靶作用于 Cys530，使野生型和突变型 ERα 失活，K_i 值分别为 1 nM 和 0.41 nM。H3B-5942 能够减少 ERα 的目标基因 GREB1 的表达。H3B-5942 具有抗癌作用，对含有 ERα^WT 或者突变型 ERα 的肿瘤细胞和动物具有抗肿瘤活性。

生物活性

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with K_is of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα^WT or ERα mutations.

体外研究

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with K_is of 1 nM and 0.41 nM, respectively.
H3B-5942 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERα^WT, various MCF7-ERαMUT lines, and the PDX-ERα^Y537S/WT line.
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERα^WT, and MCF7-LTED-ERα^Y537C lines with GI₅₀s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERα^WT or clinically frequent ERα mutations.

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

体内研究

H3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d. for 17 days) dose-dependently inhibits tumor growth in MCF7 xenograft model in athymic female nude mice.
H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERα^Y537S/WT ST941 model in athymic female nude mice.

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

Animal Model:	MCF7 xenograft model in athymic female nude mice
Dosage:	1, 3, 10, or 30 mg/kg
Administration:	P.O. once a day (q.d.×1) for 17 days
Result:	Exhibited tumor growth inhibition (TGI) on day 17 of 19%, 41%, 68%, and 83%, respectively.

体内研究

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

Animal Model:	MCF7 xenograft model in athymic female nude mice
Dosage:	1, 3, 10, or 30 mg/kg
Administration:	P.O. once a day (q.d.×1) for 17 days
Result:	Exhibited tumor growth inhibition (TGI) on day 17 of 19%, 41%, 68%, and 83%, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (168.47 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0217 mL	10.1086 mL	20.2171 mL
5 mM	0.4043 mL	2.0217 mL	4.0434 mL
10 mM	0.2022 mL	1.0109 mL	2.0217 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。-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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.21 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。