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.
For research use only. We do not sell to patients.
- CAS No.: 2991504-90-4
- Formula: C32H37F9N4O3S
- Molecular Weight:728.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
IC50=6.7 nM, DC50=0.4 nM
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Cell Line
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Type | Value | Description | References |
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| MCF7 | IC50 |
0.2 nM
Compound: G-5b
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Antiproliferative activity against wildtype human MCF7 cells assessed as inhibition of cell proliferation incubated for 6 days in presence of beta-estradiol by CellTiter-Glo assay
Antiproliferative activity against wildtype human MCF7 cells assessed as inhibition of cell proliferation incubated for 6 days in presence of beta-estradiol by CellTiter-Glo assay
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[PMID: 38007911] |
| T47D | IC50 |
0.94 nM
Compound: G-5b
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Antiproliferative activity against human T47D cells transfected with wildtype ESR1 assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay
Antiproliferative activity against human T47D cells transfected with wildtype ESR1 assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay
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[PMID: 38007911] |
| T47D | IC50 |
1 nM
Compound: G-5b
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Antiproliferative activity against human T47D cells assessed as inhibition of proliferation incubated for 6 days by CellTiter-Glo assay
Antiproliferative activity against human T47D cells assessed as inhibition of proliferation incubated for 6 days by CellTiter-Glo assay
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[PMID: 38007911] |
| T47D | IC50 |
21.06 nM
Compound: G-5b
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Antiproliferative activity against human T47D cells transfected with ESR1 D538G mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay
Antiproliferative activity against human T47D cells transfected with ESR1 D538G mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay
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[PMID: 38007911] |
| T47D | IC50 |
3.07 nM
Compound: G-5b
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Antiproliferative activity against human T47D cells transfected with ESR1 Y537S mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay
Antiproliferative activity against human T47D cells transfected with ESR1 Y537S mutant assessed as inhibition of cell proliferation incubated for 5 days by CellTiter-Glo assay
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[PMID: 38007911] |
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.
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Cell Line:T47D, MCF-7
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Concentration:100 nM
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Incubation Time:24 h
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Result:Significantly decreased the activity of ER in a dose-dependent manner.
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Cell Line:T47D, MCF-7
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Concentration:10 nM
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Incubation Time:24 h
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Result:Had antagonistic activity against ER signaling.
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Cell Line:MCF-7
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Concentration:4 nM, 20 nM, 100 nM
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Incubation Time:24 h
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Result:Blocked cells in the G1/G0 phase with a dose-dependent manner.
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Cell Line:T47D, MCF-7
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Concentration:0.2 nM for MCF-7 cells 1 nM for T47D cells
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Incubation Time:6 d
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Result:Could selectively inhibit the proliferation and migration of ER-positive breast cancer cells without affecting ER-negative ones.
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Cell Line:T74DWT, T74DY537S, T74DD538G
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Concentration:2.21 nM for T74DWT 5.94 nM for T74DY537S 58.57 nM for T74DD538G
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Incubation Time:5 d
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Result:Inhibited mutant cell proliferation in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Sprague-Dawley Rats[1]
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Dosage:30 mg/kg
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Administration:Intramuscular injection (i.m.), single dose
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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.
Chemical Information
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CAS No. 2991504-90-4
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Molecular Weight 728.71
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Formula C32H37F9N4O3S
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Estrogen receptor modulator 10 Related Classifications
HY-155406 Related Classifications
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