2052128-15-9
H3B-5942
CAS: 2052128-15-9
Molecular Formula: C31H34N4O2
2052128-15-9 - Names and Identifiers
| Name | H3B-5942 |
| Synonyms | H3B-5942 H3B-5942 free base 2-Butenamide, 4-[[2-[4-[(1E)-1-(1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]phenoxy]ethyl]amino]-N,N-dimethyl-, (2E)- |
| CAS | 2052128-15-9 |
2052128-15-9 - Physico-chemical Properties
| Molecular Formula | C31H34N4O2 |
| Molar Mass | 494.63 |
| Density | 1.157±0.06 g/cm3(Predicted) |
| Boling Point | 717.7±60.0 °C(Predicted) |
| Solubility | DMSO : 83.33 mg/mL (168.47 mM; Need ultrasonic) |
| pKa | 14.20±0.40(Predicted) |
| Storage Condition | -20°C |
| In vitro study | H3B-5942 targeting Cys530, both wild-type and mutant ERα were inactivated. Once bound to ERα, the H3B-5942 allows the DNA-binding domain of ERα to bind to the promoter and enhancer regions containing the ERE, inducing ERα to transition to a transcriptionally repressed conformation via the coactivator. In a series of containing ER alpha. |
| In vivo study | In the expression of Er alpha. |
2052128-15-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.022 ml | 10.109 ml | 20.217 ml |
| 5 mM | 0.404 ml | 2.022 ml | 4.043 ml |
| 10 mM | 0.202 ml | 1.011 ml | 2.022 ml |
| 5 mM | 0.04 ml | 0.202 ml | 0.404 ml |
Last Update：2024-01-02 23:10:35
2052128-15-9 - Reference Information
| biological activity | H3B-5942 is a selective, irreversible, ERα WT and ERα mutants were inactivated with Ki values of 1 nM and 0.41 nM, respectively. |
| Target | Value |
| ERα (Y537S) () | 0.41 nM(Ki) |
| ERα WT () | 1 nM(Ki) |
Last Update：2024-04-10 22:29:15
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Tel: 18301782025
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