Milciclib
Cat. No.：YN280019
CAS No. ：802539-81-7
| 产品名称: | Milciclib |
| CAS No.: | 802539-81-7 |
| Chemical Name: | 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide |
| Synonyms: | PHA-848125 |
| 分子量: | 460.57 |
| 分子式: | C₂₅H₃₂N₈O |
| SMILES: | O=C(NC)C1=NN(C2=C1C(C)(CC3=CN=C(N=C23)NC4=CC=C(C=C4)N5CCN(CC5)C)C)C |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Milciclib (PHA-848125) 是一种有效的CDK和Tropomyosin receptor kinase (TRK)双重抑制剂，对 cyclin A/CDK2，cyclin H/CDK7，cyclin D1/CDK4，cyclin E/CDK2，cyclin B/CDK1 和 TRKA 的IC50值分别为 45，150，160，363，398 和 53 nM。 |
| IC50和靶点: | [{name:"cyclin A/CDK2:45 nM (IC50)"},{name: "cyclin E/CDK2:363 nM (IC50)"},{name: "cyclin H/CDK7:150 nM (IC50)"},{name: "cyclin D1/CDK4:160 nM (IC50)"},{name: "cyclin B/CDK1:398 nM (IC50)"},{name: "TRKA:53 nM (IC50)"}] |
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| Solvent & Solubility: |
Brasca, M.G., Amboldi, N., Ballinari, D., et al.Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitorJ. Med. Chem.52(16),5152-5163(2009)
Caporali, S., Alvino, E., Starace, G., et al.The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compoundPharmacol. Res.61(5),437-448(2010)
Degrassi, A., Russo, M., Nanni, C., et al.Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-RasG12DLA2 lung adenocarcinoma transgenic mouse model: Evaluation by multimodality imagingMol. Cancer Ther.9(3),673-681(2010)
