2. Apoptosis
  3. MDM-2/p53
  4. 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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p53 Activator 15

p53 Activator 15 Chemical Structure

CAS No. : 3069395-29-2

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p53 Activator 15 Related Antibodies

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Description

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[1].

Application

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.

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.

p53 Activator 15 Related Antibodies
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. CL 15 mL/min/kg
Mice 10 mg/kg p.o. Cmax 5.9 μM
Mice 1 mg/kg i.v. AUC0-t 1.7 μM·h
Mice 10 mg/kg p.o. AUC0-t 15.7 μM·h
In Vivo

p53 Activator 15 (6.25-100 mg/kg, p.o., once daily for 19-28 days) exhibits excellent inhibitory activity against the proliferation of NUGC-3 transplanted tumors in mice and rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NUGC-3 transplanted tumors model established in female NuNu mice (6-8 weeks)[1]
Dosage: 25, 50 and 100 mg/kg
Administration: Oral administration (p.o.), once daily for 19 days
Result: Demonstrated good inhibitory activity against the proliferation of NUGC-3 transplanted tumors in mice at all tested doses, and exhibited dose-related properties.
Animal Model: NUGC-3 transplanted tumors model established in 7-9 week-old female B-Rag2/IL2rg knockout SD rats[1]
Dosage: 6.25, 12.5 and 25 mg/kg
Administration: Oral administration (p.o.), once daily for 28 days
Result: Demonstrated good inhibitory activity against the proliferation of NUGC-3 transplanted tumors in rats at all tested doses, and exhibited dose-related properties.
Molecular Weight

613.64

Formula

C27H27D3F4N6O4S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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p53 Activator 15 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

p53 Activator 153069395-29-2MDM-2/p53Activatorp53Y220CDNAAnti-cancerNUGC-3 xenograft mice modelHEK293 cellsNUGC-3 cellsBreast cancerStomach cancerLung cancerInhibitorinhibitorinhibit

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