H3B-5942 is a selective, irreversible and orally activeestrogen receptorcovalent antagonist, inactivates both wild-type and mutantERαby targeting Cys530, withK_is of 1 nM and 0.41 nM, respectively. H3B-5942 reducesERαtarget geneGREB1, shows potent antitumor activity both in multiple cell lines oranimalsbearingERα^WTorERαmutations^[1].

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^[1].
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 geneGREB1in MCF7-ERα^WT, various MCF7-ERαMUT lines, and the PDX-ERα^Y537S/WT line^[1].
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERα^WT, and MCF7-LTED-ERα^Y537Clines 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^WTor clinically frequent ERα mutations^[1].

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^[1].
H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERα^Y537S/WTST941 model in athymic female nude mice^[1].

494.63

Solid

C₃₁H₃₄N₄O₂

2052128-15-9

Room temperature in continental US; may vary elsewhere.

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

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。

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。