AZD-5597 is a potent CDK inhibitor with IC50 values of 2 nM for CDK1 and CDK2, respectively .
The cyclin-dependent kinases (CDKs) are serine-threonine protein kinases with roles in the regulation of the cell cycle, and also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells .
AZD-5597 is a potent imidazole pyrimidine amide CDK inhibitor. In LoVo cells, AZD-5597 exhibited high level of anti-proliferative activity with IC50 value of 0.039 μM. AZD-5597 exhibited excellent aqueous solubility ( > 50 mg/mL), photostability (t1/2 > 24 h), hydrolytic stability (pH 4-10, t1/2 > 100 days), plasma stability ( > 18 h) and the lack of CYP inhibition. The overall profile of AZD-5597 indicated that it was suitable for further development as an iv agent .
In nude mouse and rat, AZD-5597 possessed good pharmacokinetic parameters with moderate to low clearance. In nude mice implanted subcutaneously with SW620 human colon adenocarcinoma cells, AZD-5597 (15 mg/kg, dosed intermittently for 3 weeks, ip) inhibited tumour volume by 55% .
Jones CD, Andrews DM, Barker AJ, et al. The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. Bioorganic & Medicinal Chemistry Letters, 2008, 18(24): 6369-6373.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥15.65mg/mL in DMSO|
|Canonical SMILES||CC(N1C(C)=NC=C1C2=NC(NC3=CC=C(C(N4CC[[email protected]@](NC)([H])C4)=O)C=C3)=NC=C2F)C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|