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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- CAS No.: 1799430-91-3
- Formule: C28H29NO3
- Masse moléculaire:427.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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ERα |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | TGI |
78 %
Compound: 40
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Antitumor activity against human MCF7 cells xenografted in 17-beta estradiol release pellet implanted immunocompromised nude mouse assessed as tumor growth inhibition at 20 mg/kg, po administered once daily measured on day 108 relative to control
Antitumor activity against human MCF7 cells xenografted in 17-beta estradiol release pellet implanted immunocompromised nude mouse assessed as tumor growth inhibition at 20 mg/kg, po administered once daily measured on day 108 relative to control
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[PMID: 28296398] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:10 μM (single dose for % ERα remaining); dose-response series starting at 10 μM (IC50 determination)
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Incubation Time:18-24 h
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Result:Reduced ERα protein levels to 15% of control at 10 μM.
Induced ERα degradation with an IC50 of 0.9 nM in initial profiling.
Induced ERα degradation with an IC50 of 1.8 nM in a follow-up assay alongside fulvestrant.
| Species | Dose | Route | AUC0-t | CL | T1/2 (Elimination) | Cmax | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 2627 nM·h/mL | 14.9 mL/min/kg | 0.8 h | / | / | / |
| Rat[1] | 3 mg/kg | p.o. | 1586 nM·h/mL | / | / | 1199 nM | 0.3 h | 60 % |
| Dog[1] | 0.3 mg/kg | i.v. | 14347 nM·h | 2.3 mL/min/kg | 5.0 h | / | / | / |
| Dog[1] | 10 mg/kg | p.o. | 7994 mL/mg/kg | / | / | 1311 nM | 1.2 h | 56 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude mice (female, immunocompromised)[1]
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Dosage:20 mg/kg
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Administration:p.o.; once daily
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Result:Induced 78% tumor growth inhibition compared to vehicle control (day 108).
Reduced tumor ERα protein levels by 56% at 7 hours postdose and 51% at 24 hours postdose compared to vehicle control.
Caused no body weight loss in treated mice.
Chemical Information
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CAS No. 1799430-91-3
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Masse moléculaire 427.54
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Formule C28H29NO3
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
THIQ 40 Related Classifications
HY-124627 Related Classifications
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