Introduction：Basic information about CAS 38275-34-2|PK11007, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | PK11007 |
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| CAS Number | 38275-34-2 | Molecular Weight | 236.63300 |
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| Density | / | Boiling Point | / |
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| Molecular Formula | C6H5ClN2O4S | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | 5-chloro-2-methylsulfonylpyrimidine-4-carboxylic acid |
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| Synonym | More Synonyms |
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PK11007 BiologicalActivity
| Description | PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53. |
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| Related Catalog | Signaling Pathways >>Apoptosis >>MDM-2/p53Research Areas >>Cancer |
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| Target | p53[1] |
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| In Vitro | PK11007 (15-30 µM) reduces the viability of mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S). PK11007 also shows inhibitory activities against the p53 wt cancer cell lines HUH-6 and NUGC-4, as well as the fibroblast cell line WI-38 only at high concentrations (60 and 120 µM). PK11007 increases levels of p53 target genes and activates the unfolded protein response pathway. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells. PK11007 induces cell death via caspase-independent pathways. PK11007 (30, 60 µM) induces reactive oxygen species (ROS) especially in mutant p53 cells[1]. PK11007 inhibits the proliferation of a panel of 17 breast cell lines, with IC50s ranging from 2.3 to 42.2 μM[2]. |
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| Cell Assay | Cell viability is measured using the CellTiter-Fluor cell viability assay kit. Cells are seeded in 96-well plates at 7,500-15,000 cells per well and incubated overnight. Samples are prepared in medium with a twice-as-high compound (including PK11007), and DMSO concentration then added to an equivalent volume of growth medium, yielding a final DMSO concentration of 0.5%. After incubating of cells for 23 h or the respective time period, CellTiter-Fluor reagent is added to each well and incubated again for 45 min. Fluorescence is then recorded on a PHERAstar plate reader using 400/500 nm excitation/emission filters. Experiments are performed in quadruplicate[1]. |
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| References | [1]. Bauer MR, et al. 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5271-80. [2]. Synnott NC, et al. Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007. Cancer Lett. 2018 Feb 1;414:99-106 |
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Chemical & Physical Properties
| Molecular Formula | C6H5ClN2O4S |
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| Molecular Weight | 236.63300 |
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| Exact Mass | 235.96600 |
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| PSA | 105.60000 |
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| LogP | 1.31250 |
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| InChIKey | WZUPWJVRWIVWEF-UHFFFAOYSA-N |
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| SMILES | CS(=O)(=O)c1ncc(Cl)c(C(=O)O)n1 |
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| Storage condition | -20℃ |
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Safety Information
Customs
| HS Code | 2933599090 |
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| Summary | 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| 2-methanesulfonyl-5-chloro-4-pyrimidinecarboxylic acid |
| 2-methylsulfonyl-5-chloro-4-pyrimidine carboxylic acid |
| 2-methylsulfonyl-5-chloropyrimidine-4-carboxylic acid |
| 5-chloro-2-methanesulfonyl-pyrimidine-4-carboxylic acid |
| 4-carboxy-5-chloro-2-methylsulfonylpyrimidine |
| PK11007 |
