THIQ 40

THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor ERα degrader (SERD) (IC₅₀=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer^[1][2]. In Vitro:THIQ 40 (compound 40) inhibits ERα-mediated transcription in MCF-7 human breast cancer cells with an IC₅₀ of 30 nM^[1].
THIQ 40 (10 μM; 18-24 h) potently induces ERα degradation in human breast cancer MCF-7 cells^[1].
THIQ 40 inhibits insulin-mediated proliferation of MCF-7 human breast cancer cells, with an IC₅₀ of 2.1 nM at day 6^[1]. In Vivo:THIQ 40 (compound 40) (20 mg/kg; p.o.; once daily) induces 78% tumor growth inhibition and reduces tumor ERα levels by 51-56% in an estradiol-supplemented MCF-7 breast cancer xenograft model in nude mice^[1].