1366002-50-7
4-(Phenethylamino)quinazoline-6-carbonitrile
CAS: 1366002-50-7
Molecular Formula: C17H14N4
1366002-50-7 - Names and Identifiers
1366002-50-7 - Physico-chemical Properties
| Molecular Formula | C17H14N4 |
| Molar Mass | 274.32 |
| Density | 1.24±0.1 g/cm3(Predicted) |
| Boling Point | 520.0±45.0 °C(Predicted) |
| pKa | 6.47±0.50(Predicted) |
| Storage Condition | 2-8℃ |
| MDL | MFCD23703036 |
| Physical and Chemical Properties | Bioactive Senexin A is A potent, selective CDK8 inhibitor that also inhibits CDK19 with Kd values of 0.83 μm and 0.31 μm, respectively. |
| Target | Target Value CDK19 (Cell-free assay) 0.31 μM(Kd) CDK8 (Cell-free assay) 0.83 μM(Kd) |
| In vitro study | p21 can activate NF-κB-dependent transcription, while Senexin A can inhibit the NF-κB-dependent consensus promoter activity stimulated by p21. Senexin A had no effect on IPTG-induced p21, cell growth with and/or without p21, p21-induced senescence phenotype. Senexin A does not affect the inhibitory effect of p21 on gene expression, does not interfere with p21-mediated gene suppression and DNA replication in the bulk mitotic GO directory. Senexin A only inhibits p21-induced transcription without affecting other biological effects of p21. Senexin A inhibited the ATP binding sites of CDK9 and CDK19 with Kd values of 0.83 μm and 0.31 μm, respectively, and the IC50 value for inhibition of CDK8 kinase activity was 0.28 μm. In HCT116 colon cancer cells, Senexin A inhibits β-catenin dependent transcription. Senexin A does not inhibit ROCK activity, nor does it share the strong anti-endothelial cell activity of corstatin A. |
| In vivo study | CDK8/19 inhibitor Senexin A Alters (Reverses) chemotherapy-induced paracrine cancer-promoting activity in vivo, but does not inhibit the growth of reporter cells in mouse model studies, there was also no observable toxic effect. |
1366002-50-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.645 ml | 18.226 ml | 36.452 ml |
| 5 mM | 0.729 ml | 3.645 ml | 7.29 ml |
| 10 mM | 0.365 ml | 1.823 ml | 3.645 ml |
| 5 mM | 0.073 ml | 0.365 ml | 0.729 ml |
Last Update：2024-01-02 23:10:35
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