1799430-91-3
Chemical Structure
THIQ 40
- CAS No.: 1799430-91-3
- Formula:C28H29NO3
- Molecular Weight:427.54
IUPAC Name: (E)-3-(4-(6-hydroxy-2-(4-isopropylphenyl)-1-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)phenyl)acrylic acid
InChIKey: HKXVKUOGCLJVEZ-GIDUJCDVSA-N
SMILES: CC1(N(CCC=2C1=CC=C(O)C2)C3=CC=C(C(C)C)C=C3)C4=CC=C(/C=C/C(O)=O)C=C4
Biological Activity: 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].
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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. | |||||||||||||||||||||
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Keywords