NSC319726|cas 71555-25-4

Cas No.:	71555-25-4
Synonyms:	NSC-319726
SMILES:	CC(C1N=CC=CC=1)=NNC(N1CCC1)=S
Formula:	C₁₁H₁₄N₄S
M.Wt:	234.32
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.in vitro: For NSC319726, the effect was even greater as the IC50 for the 175 mutant was 8 nM while the IC50 of the WT was not reached. NSC319726 did not induce WT p53 protein levels or transcriptional activity as common cytotoxic agents such as etoposide do in vitro. NSC319726 exhibited a much higher sensitivity for the MEF-p53R172H/R172H cell line as compared to the p53+/+ and p53-/- controls. NSC319726 treatment of a MEF cell line derived from p53R172H/R172H mice resulted in a loss of PAB240 immunoflouresence staining. in vivo: At a dose of 1mg/kg, tumor growth of the H460 (p53+/+) and MDAMB468 (p53R273W) xenografts was not inhibited relative to the vehicle control whereas tumor growth was significantly inhibited in the TOV112D (p53R175H) xenografts. When we lowered the dose ten-fold to 0.1 mg/kg in the TOV112D mice, we observed only a small difference in tumor growth inhibition demonstrating both a dosage effect of the drug and a larger therapeutic window.Taken together, these findings provide in vivo evidence for allele specific p53 mutant reactivation.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
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DC47288	Teprasiran	Teprasiran (QPI-1002) is a small interfering RNA that temporarily inhibits p53-mediated cell death that underlies acute kidney injury (AKI).
DC46420	MDM2-IN-21	MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.
DC42468	p53 and MDM2 proteins-interaction-inhibitor dihydrochloride	p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an of the interaction between p53 and MDM2 proteins.
DC42467	p53 and MDM2 proteins-interaction-inhibitor (chiral)	p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an of the interaction between p53 and MDM2 proteins.
DC42132	Triglycidyl isocyanurate	Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via?p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
DC40025	Milademetan tosylate hydrate	Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
DC28687	MDM2-IN-1	MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration.
DC28442	Pifithrin-α, p-Nitro, Cyclic	Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
DC8455	Nutlin-3b	Nutlin-3b is 150-fold less potent as an inhibitor of p53-MDM2 interaction than (−)-nutlin-3, demonstrating an IC50 value of 13.6 µM.