NSC319726|cas 71555-25-4|DC Chemicals

Cas No.:	71555-25-4
Chemical Name:	NSC319726
Synonyms:	NSC 319726;Azetidinecarbothioic acid, [1-(2-pyridinyl)ethylidene] hydrazide;NSC-319726;1-AZETIDINESULFONAMIDE;32371-EP2301933A1;AG-G-46200;azetidine-1-sulphonamide;Azetidine-1-thiocarboxylic acid 2-[1-(2-pyridinyl)ethylidene]hydrazide;Azetidine-1-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide;CTK5C2671;KB-64890;QC-4196;SureCN1486989;1-Azetidinecarbothioic acid 2-[1-(2-pyridinyl)ethylidene]hydrazide;1-Azetidinecarbothioic acid;ZMC1;NSC319726;N'-(1-(Pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide;(E)-N'-(1-(pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide;MLS002703052;AZETIDINE CARBOTHIOIC ACID, [1-(2-PYRIDINYL)ETHYLIDENE]HYDRAZIDE;1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide;2597AH;s7149;SB19405;CID 5351307;CS-981;1-Azetidinecarbothioic acid, 2-[1-(2-pyridinyl)ethylidene]hydrazide;1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide NSC319726;N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide;N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide;N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide;N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide;N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide;N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide;CCG-35689;CCG-35689;CCG-35689;CCG-35689;CCG-35689;CCG-35689;AC-32867;AC-32867;AC-32867;AC-32867;AC-32867;AC-32867;EX-A2113;EX-A2113;EX-A2113;EX-A2113;EX-A2113;EX-A2113;BRD-K99170882-001-04-3;BRD-K99170882-001-04-3;BRD-K99170882-001-04-3;BRD-K99170882-001-04-3;BRD-K99170882-001-04-3;BRD-K99170882-001-04-3;71555-25-4;71555-25-4;71555-25-4;71555-25-4;71555-25-4;71555-25-4;HY-18634;HY-18634;HY-18634;HY-18634;HY-18634;HY-18634;BRD-K99170882-001-05-0;BRD-K99170882-001-05-0;BRD-K99170882-001-05-0;BRD-K99170882-001-05-0;BRD-K99170882-001-05-0;BRD-K99170882-001-05-0;LS-13960;LS-13960;LS-13960;LS-13960;LS-13960;1973511-06-6;LS-13960;1973511-06-6;1973511-06-6;1973511-06-6;1973511-06-6;AKOS024458479;1973511-06-6;AKOS024458479;AKOS024458479;AKOS024458479;AKOS024458479;CS-3542;AKOS024458479;CS-3542;CS-3542;CS-3542;CS-3542;BRD-K99170882-001-01-9;CS-3542;BRD-K99170882-001-01-9;BRD-K99170882-001-01-9;BRD-K99170882-001-01-9;BRD-K99170882-001-01-9;CHEMBL1976486;BRD-K99170882-001-01-9;CHEMBL1976486;CHEMBL1976486;CHEMBL1976486;CHEMBL1976486;WCA55525;CHEMBL1976486;WCA55525;WCA55525;WCA55525;WCA55525;AS-56104;WCA55525;AS-56104;AS-56104;SCHEMBL17975335;AS-56104;AS-56104;AS-56104;SCHEMBL17975335;SCHEMBL17975335;SCHEMBL17975335;SCHEMBL17975335;SCHEMBL17975335
SMILES:	S=C(N([H])/N=C(\C([H])([H])[H])/C1=C([H])C([H])=C([H])C([H])=N1)N1C([H])([H])C([H])([H])C1([H])[H]
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
DC73117	BAY 1892005	BAY 1892005 is a small molecule that modulate mutant p53 condensation and nuclear accumulation, binds covalently to mutant p53R175H and p53Y220C and shows stabilization of p53WT and p53Y220C, exhibits anti-proliferative activity in a set of cell lines wit
DC8599	SP 141	SP 141 is a cell-permeable inhibitor of Mdm2 (Ki = 28 nM).
DC9506	SJ-172550	SJ-172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.
DC8144	Pifithrin-β (hydrobromide)	Pifithrin-β HBr (Cyclic Pifithrin-α HBr) is a potent p53 inhibitor with IC50 of 23 uM in an antiproliferative assay in the human ovarian carcinoma cell line, IGROV-1.
DC8454	Nutlin-3a	Nutlin-3a is arbitrarily referred to as enantiomer a because it appears as the first peak from chiral purification of racemic nutlin-3 and its absolute stereocenter assignment is not known.
DC3125	Nutlin-3	Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
DC8746	NSC319726	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.
DC10957	MB725	MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM).
DC11726	Milademetan	Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
DC11837	RO-5963	RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.