1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. 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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CDD-1274

CDD-1274 Chemical Structure

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Description

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[1].

IC50 & Target

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.

Cell Viability Assay[1]

Cell Line: T47D parental, T47D Y537S
Concentration: 0 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 0 h, 6 h, 24 h, 48 h
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.
Molecular Weight

567.57

Formula

C28H33F4N3O5

SMILES

O=C(NC)CCOCCC(N1CC(C2NCC3=CC(C4=CC(O)=CC=C4OC(F)(F)F)=CC=C3F)CCC2C1)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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CDD-1274
Cat. No.:
HY-179510
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