1799430-91-3
1799430-91-3 structure
- Name: THIQ40
- Chemical Name: THIQ 40
- CAS Number: 1799430-91-3
- Molecular Formula: C28H29NO3
- Molecular Weight: 427.544
- Create Date: 2020-01-12 00:29:06
- Modify Date: 2024-02-25 17:49:48
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THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation); potently inhibits insulin driven proliferation in MCF-7 cells with IC50 of 2.1 nM, downregulate ERα protein levels and inhibit MCF-7 proliferation in an estradiol-independent manner; demonstrated SERD activity at tolerated and efficacious exposures in vivo.
| Name | THIQ 40 |
|---|
| Description | THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation); potently inhibits insulin driven proliferation in MCF-7 cells with IC50 of 2.1 nM, downregulate ERα protein levels and inhibit MCF-7 proliferation in an estradiol-independent manner; demonstrated SERD activity at tolerated and efficacious exposures in vivo. |
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| References | References 1. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818. View Related Products by Target Estrogen Receptor/ERR |
| Molecular Formula | C28H29NO3 |
|---|---|
| Molecular Weight | 427.544 |