ZM484
ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.
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- Formel: C67H72Cl2F2N6O15S2
- Molecular Weight:1374.35
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Speicherung:
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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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
ZM484 (72 h) shows potent antiproliferative activity against three cancer cell lines HCT116, SJSA-1, and A549 with IC50 values of 0.03, 0.97, and 0.11 μM, respectively[1].
ZM484 (1.56-50 μM, 72 h) exhibits minimal cytotoxicity towards the noncancerous MRC-5 cell line[1].
ZM484 (3.125-100 μM, 30 min) shows no hemolytic activity at a concentration of 100 μM[1].
ZM484 (50 μM, 0-24 h) maintains an amount concentration of over 95% within 24 h, and exhibits excellent stability even in acidic buffer solutions with pH values of 2 or 5[1].
ZM484 (25-100 nM, 8 days) significantly reduces the colony formation ability of HCT116 cells[1].
ZM484 (0.195-200 μM, 15 min) inhibits TOP1 activity in a concentration-dependent manner, retaining efficacy at concentrations as low as 0.195 μM[1].
ZM484 (50-100 nM, 4 h) upregulates p53 and MDM2 protein levels in a concentration-dependent manner[1].
ZM484 (10-40 nM, 24 h) effectively induces cell cycle arrest in HCT116 cells in the S and G2 phases[1].
ZM484 (10-640 nM, 48 h) exhibits a potent, concentration-dependent proapoptotic effect in HCT116 cells, which is concomitant with a dose-dependent decrease in the expression levels of caspase-3, Bcl-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:25, 50, and 100 nM
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Incubation Time:8 days
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Result:Significantly reduced the colony formation ability of HCT116 cells at concentrations of 25, 50, and 100 nM.
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Cell Line:HCT116 cells
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Concentration:50 and 100 nM
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Incubation Time:4 h
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Result:Increased p53 and MDM2 protein levels in a concentration-dependent manner.
Exhibited more activity than Idasanutlin (HY-15676) at 50 and 100 nM for p53 protein upregulation.
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Cell Line:HCT116 cells
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Concentration:10 and 40 nM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in the S phase (29.8% and 43.3% at 10 and 40 nM, respectively) and G2 phase (20.9% and 28.3%) cell populations.
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Cell Line:HCT116 cells
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Concentration:40, 160, and 640 nM
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Incubation Time:48 h
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Result:Induced significant apoptosis in a concentration-dependent manner, with apoptotic rates of 11.6%, 16.8%, and 25.8% at concentrations of 40, 160, and 640 nM, respectively.
Induced apoptosis more effectively than Idasanutlin or the vehicle control.
Decreased the expression levels of caspase-3, Bcl-2 in a dose-dependent manner.
| Species | Dose | Route | AUCall | AUCinf | T1/2 | CL | Vss | MRTINF_obs |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 2600 ng·h/mL | 2799 ng·h/mL | 1.65 h | 30.1 mL/min/kg | 1339 mL/kg | 0.73 h |
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 (4-6 weeks) subcutaneously injected with HCT116 cells[1]
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Dosage:10 mg/kg
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Administration:i.p., every other day for 12 days
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Result:Exhibited the highest tumor growth inhibition (TGI of 81.07%) among the tested groups, surpassing the positive controls Idasanutlin (25 mg/kg, i.g., qd, TGI = 68.59%) and Irinotecan (HY-16562) (50 mg/kg, i.p., qw, TGI = 64.01%).
Chemical Information
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Molecular Weight 1374.35
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Formel C67H72Cl2F2N6O15S2
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SMILES
O=C1C2=C(C=C3C4=NC5=CC=CC=C5C=C4CN31)[C@](OC(OCCSSCCOC(CCOCCOCCOCCOCCNC(C6=CC(OC)=C(NC([C@@H]([C@@H]([C@]7(C8=C(C=C(C=C8)Cl)F)C#N)C9=CC=CC(Cl)=C9F)N[C@H]7CC(C)(C)C)=O)C=C6)=O)=O)=O)(C(OC2)=O)CC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ZM484 Related Classifications
HY-178036 Related Classifications
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