4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]
PHA-848125
CAS: 802539-81-7
Molecular Formula: C25H32N8O
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h] - Names and Identifiers
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h] - Physico-chemical Properties
| Molecular Formula | C25H32N8O |
| Molar Mass | 460.57 |
| Density | 1.33 |
| Melting Point | 190 °C |
| pKa | 14.44±0.40(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | PHA-848125 potently inhibits cyclin A/CDK2 with an IC50 of 45 nM and is PHA-84812 A competitive inhibitor of ATP. PHA-848125 also inhibited cyclin H/CDK7,cyclin D1/CDK4,p35/CDK5,cyclin E/CDK2, and cyclin B/CDK1 activities with IC50 of 0.15, 0.16, 0.265, respectively, 0.363, 0.398 M. When PHA-848125 acts on most PHA-848125-sensitive cell lines, the cell cycle is induced to stop in G1 phase, and this inhibition is concentration-dependent. PHA-848125 also disrupts the phosphorylation of retinal glioma proteins at specific sites of CDK2 and CDK4, reduces retinal glioma protein and cyclin A levels, and enhances p21(Cip1), p27(Kip1) and p53 expression. The combination of TMZ,BG and PHA-848125 produces a synergistic effect on cell growth. |
| In vivo study | PHA-848125 can be highly effective in the A2780 human ovarian cancer model. PHA-848125, K-Ras(G12D)LA2 mice were treated twice a day at a dose of 40 mg/kg for 10 days. At the end of the treatment, tumor growth was significantly inhibited. In a variety of human xenograft models, carcinogen-induced tumor models, and invasive primary leukemia models, oral treatment of PHA-848125, with significant anti-cancer activity. |
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h] - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.171 ml | 10.856 ml | 21.712 ml |
| 5 mM | 0.434 ml | 2.171 ml | 4.342 ml |
| 10 mM | 0.217 ml | 1.086 ml | 2.171 ml |
| 5 mM | 0.043 ml | 0.217 ml | 0.434 ml |
Last Update：2024-01-02 23:10:35
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h] - Reference Information
| biological activity | Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor that acts on CDK2, the IC50 is 45 nM and is more than 3-fold more selective for CDK2 than CDK1, 2, 4, 5 and 7. Milciclib (PHA-848125) can induce cell death by autophagy. Phase 2. |
| Target | Value |
| CDK2/CyclinA (Cell-free assay) | 45 nM |
| TrkA (Cell-free assay) | 53 nM |
| CDK7/CyclinH (Cell-free assay) | 150 nM |
| CDK4/CyclinD1 (Cell-free assay) | 160 nM |
| CDK5/p35 (Cell-free assay) | 265 nM |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: PHA-848125 Visit Supplier Webpage Request for quotationCAS: 802539-81-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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