ZN-c5
ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer.
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- No. CAS: 2136606-87-4
- Fòrmula: C26H24F2N2O2
- Peso molecular:434.48
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
ZN-c5 (100 nM, 24 h) induces ERα degradation in breast cancer cell lines (MCF-7, ZR-75-1, CAMA-1, HCC1500 and HCC1428 cells)[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, ZR-75-1, CAMA-1, HCC1500 and HCC1428 cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Induced ERα degradation in breast cancer cell lines.
| Species | Dose | Route | AUC | Cmax | F | CL | T1/2 | Vdss |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 10 mg/kg | p.o. | 2004 μM·h | 68 μM | 88 % | / | / | / |
| Dog[1] | 3 mg/kg | i.v. | 732 μM·h | / | / | 0.18 μM | 21 h | 0.33 L/kg |
| Mice[1] | 10 mg/kg | p.o. | 65 μM·h | 10.8 μM | 74 % | / | / | / |
| Mice[1] | 3 mg/kg | i.v. | 26 μM·h | / | / | 4.4 mL/min/kg | 2.9 h | 1.2 L/kg |
| Rat[1] | 10 mg/kg | p.o. | 283 μM·h | 33 μM | 88 % | / | / | / |
| Rat[1] | 3 mg/kg | i.v. | 96 μM·h | / | / | 1.2 mL/min/kg | 4.2 h | 0.48 L/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice were inoculated subcutaneously on the second right mammary fat pad with the single cell suspension of 95% viable tumor cells (1.5 × 107) in 200 μL medium Matrigel mixture (1:1 ratio) without serum[1]
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Dosage:1, 5, 40 mg/kg
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Administration:p.o. once daily for 28 days
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Result:Resulted in complete tumor growth inhibition at 5 mg/kg.
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Animal Model:Female athymic BALB/c nude mice were implanted with a single cell suspension of 1.5 × 106 WHIM20 cells[1]
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Dosage:40 mg/kg
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Administration:p.o. once daily for 90 days
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Result:Induced tumor growth inhibition and showed no loss in body weight.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2136606-87-4
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Peso molecular 434.48
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Fòrmula C26H24F2N2O2
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SMILES
FC1=CC(/C=C/C(O)=O)=CC(F)=C1[C@H]2N([C@@H](CC3=C2NC4=CC=CC=C43)C)C56CC(C6)C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZN-c5 Related Classifications
HY-175260 Related Classifications
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