| Identification | Back Directory | [Name]
PHA-848125 | [CAS]
802539-81-7 | [Synonyms]
Milciclib
PHA-84812
PHA-848125
PHA-848125 USP/EP/BP
PHA-848125 (Milciclib)
Milciclib (PHA-848125)
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]
N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-
4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide PHA 848125 | [Molecular Formula]
C25H32N8O | [MDL Number]
MFCD17169990 | [MOL File]
802539-81-7.mol | [Molecular Weight]
460.57 |
| Chemical Properties | Back Directory | [Melting point ]
190 °C | [density ]
1.33 | [storage temp. ]
Store at -20°C | [solubility ]
≥23.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O | [form ]
solid | [pka]
14.44±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM).1 It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7.1 PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.1,2,3 | [Uses]
PHA-848125 is a cyclin dependent kinase (CDK) inhibitor. Oral PHA-848125 showed antitumor activity via dual targeting of cyclin-dependent kinase and tropomyosin receptor kinase families in human carcinoma cell and xenografted mouse model of carcinoma. | [Enzyme inhibitor]
This cyclin kinase-directed inhibitor (FW = 460.57 g/mol; CAS 802539-81- 7, 802540-32-5 (3HCl), 1253645-38-3 (Maleic acid); Solubility: 90 mg/mL DMSO; <1 mg/mL Water), systematically named N,1,4,4-tetramethyl-8-(4- (4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h] quinazoline-3-carboxamide, targets cyclin A/CDK2 inhibitor with IC50 of 45 nM. PHA-848125-treated cells show cell cycle arrest in G1 and reduced DNA synthesis, accompanied by inhibition of pRb phosphorylation and modulation of other CDK-dependent markers. Cyclin Target Selectivity: Cdk1 (weak, if any), Cdk2 (++), Cdk3 (weak, if any), Cdk4 (weak, if any), Cdk5 (weak, if any), Cdk6 (weak, if any), Cdk7 (weak, if any), Cdk8 (weak, if any), Cdk9 (weak, if any), Cdk10 (weak, if any) | [target]
CDK2/CyclinA | [References]
1. brasca mg, 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 inhibitor. j med chem. 2009 aug 27;52(16):5152-63. |
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