CDD-1274
CDD-1274 is an ERα (Estrogen receptor α) variant inhibitor. CDD-1274 induces proteasomal degradation of ERα variants in breast cancer cell lines and causes Y537S ERα degradation. CDD-1274 potently blocks ligand-dependent and ligand-independent ER signaling in endocrine-resistant breast cancer cells. CDD-1274 can be used for the study of breast cancer.
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- 화학식: C28H33F4N3O5
- 분자량:567.57
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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ERαY537S |
ERα |
In Vitro
CDD-1274 (10 μM) effectively blocks the recruitment of SRC3 coactivator peptides to Y537S and D538G mutant ERa LBDs[1].
CDD-1274 (0-10 μM, 0-48 h) reduces the levels of WT and Y537S ERa proteins in T47D parental and T47D Y537S, accompanied by decreased expression of cyclin D1, survivin, and progesterone receptor (PR)[1].
CDD-1274 (10 μM, 24 h) reduces ERa protein levels in MCF-7 parental and MCF-7 Y537S and D538G mutants; decreases the expression of cell proliferation markers (cyclin D1, survivin, E2F1) and ER target genes (TFF1, GREB1, PR); and increases the apoptosis marker c-PARP[1].
CDD-1274 (10 μM, 24 h) degrades WT and Y537S ERa in Palbociclib-resistant MCF-7 WT and Y537S cells and inhibits the expression of cyclin D1, survivin, and TFF1[1].
CDD-1274 (10 μM, 24 h) reduces ERa and proliferation markers in ER-positive cells (such as T47D and MCF-7); in ER-negative cells (MCF-10A, HCC1954, MDA-MB-231, and VCaP), it was a pure antagonist in Ishikawa[1].
CDD-1274 (10 μM, 24 h) induces persistent ERa degradation in T47D parental and T47D Y537S[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D parental, T47D Y537S
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Concentration:0 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM
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Incubation Time:0 h, 6 h, 24 h, 48 h
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Result:Decreased levels of ERa protein in WT and Y537S were accompanied by decreased expression of cyclin D1, survivin, and progesterone receptor (PR).
ERA degradation began within 6 hours and disappeared completely within 48 hours; downstream markers (such as cyclin D1) also decreased in a time-dependent manner.
Chemical Information
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분자량 567.57
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화학식 C28H33F4N3O5
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SMILES
O=C(NC)CCOCCC(N1CC(C2NCC3=CC(C4=CC(O)=CC=C4OC(F)(F)F)=CC=C3F)CCC2C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDD-1274 Related Classifications
HY-179510 Related Classifications
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