2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. 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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THIQ 40

THIQ 40 화학구조

CAS No. : 1799430-91-3

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THIQ 40 Related Antibodies

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  • Biological Activity

  • 순도&문서

  • References

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제품 설명

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].

IC50 & Target[1]

ERα

 

Cellular Effect
Cell Line Type Value Description References
MCF7 TGI
78 %
Compound: 40
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
[PMID: 28296398]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

THIQ 40 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 10 μM (single dose for % ERα remaining); dose-response series starting at 10 μM (IC50 determination)
Incubation Time: 18-24 h
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.
Parmacokinetics
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 %
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: nude mice (female, immunocompromised)[1]
Dosage: 20 mg/kg
Administration: p.o.; once daily
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.
분자량

427.54

화학식

C28H29NO3
CAS No.
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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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THIQ 40 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

THIQ 401799430-91-3THIQ40THIQ-40Estrogen Receptor/ERRMCF-7 breast cancer xenograft modelestrogen receptor degraderMet421ERα+ breast cancerMCF-7 human breast cancer cellsERαHis524nude micehuman ERα LBDSaccharomyces cerevisiae strain LP501Inhibitorinhibitorinhibit

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상품명:
THIQ 40
Cat. No.:
HY-124627
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