AZD 5438

Bezeichnung:AZD 5438

CAS-Nr602306-29-6

Englisch Name:AZD 5438

CBNumberCB61512498

SummenformelC18H21N5O2S

Molgewicht371.46

MOL-Datei602306-29-6.mol

AZD 5438 physikalisch-chemischer Eigenschaften

Siedepunkt	655.2±65.0 °C(Predicted)
Dichte	1.31
storage temp.	Keep in dark place,Inert atmosphere,2-8°C
Löslichkeit	insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥42.1 mg/mL in EtOH
Aggregatzustand	solid
pka	4.08±0.50(Predicted)
Farbe	White to light yellow

Gefahreninformationscode (GHS)

AZD 5438 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
AZD 5438 is a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, which leads to leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts.
Definition
ChEBI: 4-(2-methyl-3-propan-2-yl-4-imidazolyl)-N-(4-methylsulfonylphenyl)-2-pyrimidinamine is a sulfonamide.
Biologische Aktivität
azd5438 is a potent small molecule inhibitor of cyclin-dependent kinase (cdk) 1, 2 and 9 with half maximal inhibitory concentration ic50 of 16 nmol/l, 6 nmol/l and 20 nmol/l respectively. azd5438 has also been found to potently inhibit the human cyclin e/cdk2 complex, the cyclin b1/cdk1 complex and the cyclin a/cdk2 complex with ic50 of 0.006 μm, 0.016 μm and 0.045 μm respectively. in previous studies, azd5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with ic50 ranging from 0.2 μmol/l to 1.7 μmol/l, in which the phosphorylation of a few proteins, including cdk substrates prb, nucleolin, protein phosphatase 1a and rna polymerase ii cooh-terminal domain, and cell cycling at g2-m, s and g1 phases were inhibited.
Lager
Desiccate at RT
Einzelnachweise
[1]camidge dr1, smethurst d, growcott j, barrass nc, foster jr, febbraro s, swaisland h, hughes a. a first-in-man phase i tolerability and pharmacokinetic study of the cyclin-dependent kinase-inhibitor azd5438 in healthy male volunteers. cancer chemother pharmacol. 2007 aug;60(3):391-8. epub 2006 nov 18.
[2]byth kf, thomas a, hughes g, forder c, mcgregor a, geh c, oakes s, green c, walker m, newcombe n, green s, growcott j, barker a, wilkinson rw. azd5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. mol cancer ther. 2009 jul;8(7):1856-66. doi: 10.1158/1535-7163.mct-08-0836. epub 2009 jun 9.

AZD 5438 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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