PROTAC ERα Degrader-11
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)).
For research use only. We do not sell to patients.
- Formula: C51H47F3N4O12S
- Molecular Weight:997.00
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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ERα |
ERβ |
PROTAC ERα Degrader-11 (Compound W2) (96 h) exhibits excellent cell inhibitory activity with IC50 values of 0.19 μM (MCF-7), 1.40 μM (MCF-7EGFR), 4.31 μM (MCF-7D538G) and 9.29 μM (MCF-7Y537S)[1].
PROTAC ERα Degrader-11 (10 μM, 0-24 h) degrades ERα in MCF-7 cells in a time-dependent manner within 24 h, which is reduced after the addition of the ERα ligand (OBHSA) (HY-167701) or CRBN ligand[1].
PROTAC ERα Degrader-11 (0.5-10 μM, 24 h) does not degrade ERβ in PC9 cells[1].
PROTAC ERα Degrader-11 (0-80 μM, 10-360 min) exhibits a concentration-dependent and time-dependent proportional increase in fluorescence intensity[1].
PROTAC ERα Degrader-11 (1-20 μM, 48 h) induces G2/M phase arrest and induces apoptosis in MCF-7 cells[1].
PROTAC ERα Degrader-11 (10 μM, 0-60 min) exhibits high photostability in the presence of ERα[1].
PROTAC ERα Degrader-11 (0.1-20 μM) does not induce significant damage to the blood cell membranes in SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:1, 10 μM
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Incubation Time:48 h
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Result:Induced G2/M phase arrest dose-dependently in MCF-7 cells.
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Cell Line:MCF-7 cells
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Concentration:10, 20 μM
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Incubation Time:48 h
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Result:Induced apoptosis dose-dependently in MCF-7 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/C nude mice (5 weeks)[1]
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Dosage:500 mg/kg
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Administration:i.p. for single dose
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Result:Showed no treatment-related mortality or clinical signs of toxicity (including piloerection, lethargy, or neurological abnormalities).
Showed no abnormality of body weight changed.
Chemical Information
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Molecular Weight 997.00
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Formula C51H47F3N4O12S
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SMILES
O=S(N(C1=CC=C(OCC(NCCCCCCOC2=CC3=CC=CC(C4=O)=C3C(C(N4C(C5=O)CCC(N5)=O)=O)=C2)=O)C=C1)CC(F)(F)F)([C@H]6[C@@H]7C(C8=CC=C(O)C=C8)=C(C9=CC=C(O)C=C9)[C@@H](O7)C6)=O
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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)
PROTAC ERα Degrader-11 Related Classifications
HY-174870 Related Classifications
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