THIQ 40

Research use only, not for human use.

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 (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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THIQ40

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

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1799430-91-3

427.544

C28H29NO3

>98% (HPLC)

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CC(C)C1=CC=C(C=C1)N2CCC3=C(C2(C)C4=CC=C(C=C4)C=CC(=O)O)C=CC(=C3)O

(E)-3-(4-(6-Hydroxy-2-(4-isopropylphenyl)-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)phenyl)acrylic Acid

(-20℃)

With Ice Pack

≥ 2 years