1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. ERα degrader-2

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research.

For research use only. We do not sell to patients.

ERα degrader-2 Chemical Structure

ERα degrader-2 Chemical Structure

CAS No. : 2235396-63-9

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Description

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research[1].

IC50 & Target[1]

ERα

4.6 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
ES-2 IC50
17.1 nM
Compound: D24
Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay
Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay
[PMID: 34056898]
MCF7 IC50
0.27 nM
Compound: D24
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay
[PMID: 34056898]
In Vitro

ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells[1].

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

In Vivo

ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice[1].
ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%[1].

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

Animal Model: MCF-7 human breast cancer xenograft model in nude mice[1]
Dosage: 2 mg/kg; 6 mg/kg
Administration: Oral administration; 2-6 mg/kg; QD; 21 days
Result: Exhibited in vivo efficacy in breast cancer xenograft model.
Molecular Weight

492.53

Formula

C29H27F3N2O2

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

CC(C)(F)CN1[C@@](C2=C(C=C(C3=CC=C(C=C3)C(O)=O)C=C2F)F)([H])C4=C(C[C@H]1C)C5=CC=CC=C5N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)

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Purity & Documentation
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ERα degrader-2 Related Classifications

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  • 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.

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ERα degrader-2
Cat. No.:
HY-132194
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