Introduction：Basic information about CAS 71555-25-4|NSC 319726, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | NSC 319726 |
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| CAS Number | 71555-25-4 | Molecular Weight | 234.321 |
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| Density | 1.3±0.1 g/cm3 | Boiling Point | 367.7±34.0 °C at 760 mmHg |
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| Molecular Formula | C11H14N4S | Melting Point | / |
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| MSDS | / | Flash Point | 176.2±25.7 °C |
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Names
| Name | Azetidinecarbothioic acid, [1-(2-pyridinyl)ethylidene] hydrazide |
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| Synonym | More Synonyms |
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NSC 319726 BiologicalActivity
| 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.IC50 value: 8 nM [1]Target: mutant p53R175 reactivatorin vitro: For NSC319726, the effect was even greater as the IC50for 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 aloss 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. |
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| Related Catalog | Signaling Pathways >>Apoptosis >>MDM-2/p53Research Areas >>Cancer |
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| References | [1]. Yu X, et al. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-25. |
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Chemical & Physical Properties
| Density | 1.3±0.1 g/cm3 |
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| Boiling Point | 367.7±34.0 °C at 760 mmHg |
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| Molecular Formula | C11H14N4S |
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| Molecular Weight | 234.321 |
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| Flash Point | 176.2±25.7 °C |
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| Exact Mass | 234.093918 |
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| PSA | 72.61000 |
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| LogP | 0.17 |
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| Vapour Pressure | 0.0±0.8 mmHg at 25°C |
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| Index of Refraction | 1.659 |
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| InChIKey | XDHBUMNIQRLHGO-UKTHLTGXSA-N |
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| SMILES | CC(=NNC(=S)N1CCC1)c1ccccn1 |
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| Storage condition | -20°C |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- CM4387000
- CHEMICAL NAME :
- 1-Azetidinethiocarboxylic acid, (1-(2-pyridyl)ethylidene)hydrazide
- CAS REGISTRY NUMBER :
- 71555-25-4
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 1
- MOLECULAR FORMULA :
- C11-H14-N4-S
- MOLECULAR WEIGHT :
- 234.35
- WISWESSER LINE NOTATION :
- T6NJ BY1&UNMYUS&- AT4NTJ
HEALTH HAZARD DATAACUTE TOXICITY DATAMUTATION DATA - TYPE OF TEST :
- DNA inhibition
- TEST SYSTEM :
- Microorganism - not otherwise specified
- DOSE/DURATION :
- 2460 ug/L
- REFERENCE :
- AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 18,317,1980
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Synonyms
| N'-[(1E)-1-(2-Pyridinyl)ethylidene]-1-azetidinecarbothiohydrazide |
| Azetidine-1-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide |
| 1-Azetidinecarbothioic acid, 2-[(1E)-1-(2-pyridinyl)ethylidene]hydrazide |
| Azetidine-1-thiocarboxylic acid 2-[1-(2-pyridinyl)ethylidene]hydrazide |
| 1-AZETIDINESULFONAMIDE |
| azetidine-1-sulphonamide |
| NSC319726 |
| 1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide |
