PHA-848125

Bezeichnung:PHA-848125

CAS-Nr802539-81-7

Englisch Name:PHA-848125

CBNumberCB92500952

SummenformelC25H32N8O

Molgewicht460.57

MOL-Datei802539-81-7.mol

PHA-848125 physikalisch-chemischer Eigenschaften

Schmelzpunkt	190 °C
Dichte	1.33
storage temp.	Store at -20°C
Löslichkeit	≥23.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Aggregatzustand	solid
pka	14.44±0.40(Predicted)
Farbe	Light yellow to yellow

Gefahreninformationscode (GHS)

PHA-848125 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC₅₀ = 45 nM). It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7. PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.
Verwenden
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.
Enzyminhibitor
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
Einzelnachweise
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.

PHA-848125 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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