38275-34-2
38275-34-2 structure
- Name: PK11007
- Chemical Name: 5-chloro-2-methylsulfonylpyrimidine-4-carboxylic acid
- CAS Number: 38275-34-2
- Molecular Formula: C6H5ClN2O4S
- Molecular Weight: 236.63300
- Catalog: Signaling Pathways Apoptosis MDM-2/p53
- Create Date: 2019-01-02 18:23:12
- Modify Date: 2024-01-13 11:28:55
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PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.
| Name | 5-chloro-2-methylsulfonylpyrimidine-4-carboxylic acid |
|---|---|
| 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 |
| Description | PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53. |
|---|---|
| Related Catalog | |
| Target |
p53[1] |
| 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]. |
| 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]. |
| References |
| Molecular Formula | C6H5ClN2O4S |
|---|---|
| Molecular Weight | 236.63300 |
| Exact Mass | 235.96600 |
| PSA | 105.60000 |
| LogP | 1.31250 |
| Storage condition | -20℃ |
| HS Code | 2933599090 |
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| Precursor 1 | |
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| DownStream 1 | |
| HS Code | 2933599090 |
|---|---|
| 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% |