Cas No.: | 1799430-91-3 |
Chemical Name: | (E)-3-(4-(6-Hydroxy-2-(4-isopropylphenyl)-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)phenyl)acrylic Acid |
Synonyms: | THIQ 40 |
SMILES: | C(O)(=O)/C=C/C1=CC=C(C(C)2C3=C(C=C(O)C=C3)CCN2C2=CC=C(C(C)C)C=C2)C=C1 |
Formula: | C28H29NO3 |
M.Wt: | 427.544 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |