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Chemical Structure : THIQ 40
Catalog No.: PC-35861Not For Human Use, Lab Use Only.
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).
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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).
THIQ 40 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.
THIQ 40 demonstrated SERD activity at tolerated and efficacious exposures in vivo.
| M.Wt | 427.544 | |
| Formula | C28H29NO3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818.
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