p53 Activator 15
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer.
For research use only. We do not sell to patients.
- CAS No.: 3069395-29-2
- Formula: C27H27D3F4N6O4S
- Molecular Weight:613.64
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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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Help & FAQs
Biological Activity
p53 Activator 15 (Compound 2) significantly suppresses NUGC-3 cells proliferation with an IC50 of 58 nM[1].
p53 Activator 15 has relatively weak or no significant inhibitory activity on CYP series enzymes and hERG. It also exhibits high metabolic stability in human/rat/mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NUGC-3 transplanted tumors model established in female NuNu mice (6-8 weeks)[1]
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Dosage:25, 50 and 100 mg/kg
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Administration:Oral administration (p.o.), once daily for 19 days
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Result:Demonstrated good inhibitory activity against the proliferation of NUGC-3 transplanted tumors in mice at all tested doses, and exhibited dose-related properties.
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Animal Model:NUGC-3 transplanted tumors model established in 7-9 week-old female B-Rag2/IL2rg knockout SD rats[1]
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Dosage:6.25, 12.5 and 25 mg/kg
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Administration:Oral administration (p.o.), once daily for 28 days
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Result:Demonstrated good inhibitory activity against the proliferation of NUGC-3 transplanted tumors in rats at all tested doses, and exhibited dose-related properties.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 3069395-29-2
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Molecular Weight 613.64
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Formula C27H27D3F4N6O4S
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SMILES
O=C(NS(C)(=O)=O)C1=CC=C(NCC#CC2=C(N3C=CC=C(C3=C2)N[C@@H]4CCN(C[C@@H]4F)C)CC(F)(F)F)C(OC([2H])([2H])[2H])=N1
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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)
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