THIQ40

Modify Date: 2024-02-25 17:49:48

THIQ40 Structure
THIQ40 structure
Common Name THIQ40
CAS Number 1799430-91-3 Molecular Weight 427.544
Density N/A Boiling Point N/A
Molecular Formula C28H29NO3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of THIQ40


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.

 Names

Name THIQ 40

 THIQ40 Biological Activity

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.
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

 Chemical & Physical Properties

Molecular Formula C28H29NO3
Molecular Weight 427.544
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