2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Estrogen Receptor/ERR Caspase Bcl-2 Family
  4. Estrogen receptor modulator 10

Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research.

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Estrogen receptor modulator 10

Estrogen receptor modulator 10 Chemical Structure

CAS No. : 2991504-90-4

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Estrogen receptor modulator 10 Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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Description

Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research[1].

IC50 & Target

IC50=6.7 nM, DC50=0.4 nM
In Vitro

Estrogen receptormodulator 10 (20-100 nM, 2-48 h) significantly reduces ER activity in T47D cells in a dose-dependent manner, and degrades ER in MCF-7 cells later than in T47D cells[1].
Estrogen receptormodulator 10 (10 nM, 24 h) can reduce the growth regulation of TFF-1 (trefoil factor 1), PgR (progesterone receptor) and GRBE1 (GRBE1) produced by E2 stimulation in MCF-7 and T47D cells by estrogen in breast cancer 1)[1].
Estrogen receptormodulator 10 (4-100 nM, 24 h) induces apoptosis in MCF-7 cells, and significantly enhances the activity of caspase-3 and caspase-9 in MCF-7 cells[1].
Estrogen receptormodulator 10 (4-100 nM, 24 h) can inhibit the expression of G1/G0 phase protein in MCF-7 cells[1].
Estrogen receptormodulator 10 (0.2-1 nM, 6 d) significantly inhibits the proliferation of MCF-7 and T47D cells mediated by E2[1].
Estrogen receptormodulator 10 (4-100 nM, 24 h) significantly reduces the levels of cell migration and proliferating nuclear antigen in MCF-7 cells[1].
Estrogen receptormodulator 10 (20-100 nM, 24 h) reduces ER in cytoplasm and nucleus in MCF-7 cells, promoting the transfer of ER from nucleus to cytoplasm. ER is rapidly degraded through proteasome pathway without affecting the expression of corresponding mRNA[1].

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

Estrogen receptor modulator 10 Related Antibodies

Cell Viability Assay[1]

Cell Line: T47D, MCF-7
Concentration: 100 nM
Incubation Time: 24 h
Result: Significantly decreased the activity of ER in a dose-dependent manner.

RT-PCR[1]

Cell Line: T47D, MCF-7
Concentration: 10 nM
Incubation Time: 24 h
Result: Had antagonistic activity against ER signaling.

Cell Cycle Analysis[1]

Cell Line: MCF-7
Concentration: 4 nM, 20 nM, 100 nM
Incubation Time: 24 h
Result: Blocked cells in the G1/G0 phase with a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: T47D, MCF-7
Concentration: 0.2 nM for MCF-7 cells
1 nM for T47D cells
Incubation Time: 6 d
Result: Could selectively inhibit the proliferation and migration of ER-positive breast cancer cells without affecting ER-negative ones.

Cell Proliferation Assay[1]

Cell Line: T74DWT, T74DY537S, T74DD538G
Concentration: 2.21 nM for T74DWT
5.94 nM for T74DY537S
58.57 nM for T74DD538G
Incubation Time: 5 d
Result: Inhibited mutant cell proliferation in a dose-dependent manner.
In Vivo

Estrogen receptormodulator 10 (30 mg/kg Intramuscular injection (i.m.), single dose) shows favorable pharmacokinetic properties in female Sprague-Dawley mice[1].

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

Animal Model: Female Sprague-Dawley Rats[1]
Dosage: 30 mg/kg
Administration: Intramuscular injection (i.m.), single dose
Result: Showed apparent distribution volume (Vz_F_obs≈1600 L) was nearly 1.3 times smaller than that of fulvestrant (Vz_F_obs≈2100 L), and most drugs could be widely distributed from blood to target tissues and organs.
Molecular Weight

728.71

Formula

C32H37F9N4O3S
CAS No.
SMILES

FC(C=C(NC1CN(CCCS(CCCC(F)(F)C(F)(F)F)(=O)=O)C1)C=C2F)=C2[C@H]3N(CC(F)(F)CO)[C@H](C)CC4=C3NC5=CC=CC=C54
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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
References
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Estrogen receptor modulator 10 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:

Estrogen receptor modulator 102991504-90-4Estrogen receptor modulator10Estrogen receptor modulator-10Estrogen Receptor/ERRCaspaseBcl-2 FamilyTumorAntagonistDegraderPharmacokineticsPharmacodynamics propertiesMCF-7T47DFemale Sprague-Dawley RatsBreast cancerInhibitorinhibitorinhibit

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