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.
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- CAS No.: 3069395-29-2
- 화학식: C27H27D3F4N6O4S
- 분자량:613.64
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
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.
Parmacokinetics
In Vivo
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.
- Protocol for Electrophoretic Mobility Shift Assay (EMSA)
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
신청
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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분자량 613.64
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
p53 Activator 15 Related Classifications
HY-175318S Related Classifications
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