NCP07
NCP07 is a PROTAC degrader targeting the coactivator-binding site (CBS) of ERα. NCP07 induces the formation of the ERα-NCP07-VHL ternary complex and promotes ERα degradation via the ubiquitin-proteasome system. NCP07 induces apoptosis and cell cycle arrest in endocrine therapy-resistant breast cancer cells. NCP07 inhibits the proliferation of wild-type and ESR1-mutant breast cancer cells. NCP07 is applicable to breast cancer-related research.
(Pink: ERα Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker (HY-N0067)).
For research use only. We do not sell to patients.
- Formula: C58H72N8O13S
- Molecular Weight:1121.30
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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
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- References
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Help & FAQs
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Biological Activity
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ERα |
NCP07 potently inhibits the proliferation of wild-type MCF-7 breast cancer cells with an IC50 of 0.25 μM; it potently inhibits the proliferation of endocrine-resistant LCC2 breast cancer cells with an IC50 of 1.01 μM; and it potently inhibits the proliferation of ESR1-mutant MCF-7EGFR, MCF-7D538G and MCF-7Y537S breast cancer cells, with IC50 values ranging from 0.13 to 1.22 μM[1].
NCP07 (5-10 μM; 24 h) selectively degrades ERα in wild-type MCF-7 breast cancer cells[1].
NCP07 (1-10 μM; 24 h) selectively degrades ERα in endocrine-resistant LCC2 breast cancer cells in a concentration-dependent manner[1].
NCP07 (1-10 μM; 12 h) selectively degrades ERα in a concentration-dependent manner in T47D breast cancer cells as well as ESR1-mutated MCF-7EGFR, MCF-7D538G and MCF-7Y537S breast cancer cells[1].
NCP07 (5 μM) induces ERα degradation in endocrine-resistant LCC2 breast cancer cells via specific binding to the ERα coactivator binding site (CBS); it can induce the formation of a stable ERα-NCP07-VHL ternary complex in endocrine therapy-resistant LCC2 breast cancer cells through specific binding to ERα CBS[1].
NCP07 (0.1-20 μM; 72 h) induces apoptosis in endocrine-resistant LCC2 breast cancer cells in a concentration-dependent manner[1].
NCP07 (1-10 μM; 72 h) activates the apoptotic signaling pathway in endocrine-resistant LCC2 breast cancer cells, inducing caspase-3 activation and PARP cleavage[1].
NCP07 (1-20 μM; 48 h) selectively induces G1-phase cell cycle arrest in endocrine-resistant LCC2 breast cancer cells in vitro in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type MCF-7 breast cancer cells
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Concentration:5, 10 μM
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Incubation Time:24 h
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Result:Induced ~20% degradation of ERα at 5 μM.
Induced ~75% degradation of ERα at 10 μM.
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Cell Line:endocrine-resistant LCC2 breast cancer cells
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Concentration:1, 5, 10 μM
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Incubation Time:24 h
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Result:Induced degradation of ERα.
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Cell Line:ESR1-mutated breast cancer cells (MCF-7EGFR, MCF-7D538G, MCF-7Y537S) and T47D breast cancer cells
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Concentration:1, 5, 10 μM
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Incubation Time:12 h
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Result:Induced graded ERα degradation in four cell strains: T47D (60/80/90%), MCF-7EGFR (50/70/80%), MCF-7D538G (30/50/70%), MCF-7Y537S (20/40/60%) at 1, 5, 10 μM.
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Cell Line:endocrine-resistant LCC2 breast cancer cells
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Concentration:10 μM (NCP07); 5 μM (E2 co-incubated); 3 μM (KP1490 co-incubated)
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Incubation Time:12 h
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Result:Induced significant co-localization of ERα and VHL (orange-yellow merged fluorescence) in the nucleus.
Co-incubation with KP1490 inhibited ERα-VHL co-localization.
Co-incubation with E2 did not inhibit ERα-VHL co-localization.
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Cell Line:endocrine-resistant LCC2 breast cancer cells
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Concentration:0.1, 1, 10, 20 μM
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Incubation Time:72 h
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Result:Induced concentration-dependent apoptosis in LCC2 cells.
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Cell Line:endocrine-resistant LCC2 breast cancer cells
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Concentration:1, 5 μM (PRAP)
1, 5, 10 μM (Caspase-3)
5 μM (cleaved forms) -
Incubation Time:72 h
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Result:Induced concentration-dependent reduction in full-length PARP protein levels.
Induced concentration-dependent reduction in full-length caspase-3 protein levels.
Induced corresponding concentration-dependent increases in cleaved-PARP levels.
Induced corresponding concentration-dependent increases in cleaved-caspase-3 levels.
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Cell Line:wild-type MCF-7 and endocrine-resistant LCC2 breast cancer cells
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Concentration:1, 10, 20 μM
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Incubation Time:48 h
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Result:Showed no significant effect on cell cycle distribution in MCF-7 cells.
Induced concentration-dependent G1 phase arrest in LCC2 cells.
At 20 μM, 87.80% of LCC2 cells were in G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1121.30
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Formula C58H72N8O13S
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SMILES
C[C@@H](C1=CC=C(C2=C(C)N=CS2)C=C1)NC([C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(CCCNC(C(C=C4)=CC(OCC(C)C)=C4NC(C(C=C5)=CC(OCC(C)C)=C5NC(C6=CC(OCCO)=C([N+]([O-])=O)C=C6)=O)=O)=O)=O)=O)=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)
NCP07 Related Classifications
HY-187225 Related Classifications
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