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AZD-5597

In stock
Catalog No.
B5926
Potent CDK inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$490.00
In stock
5mg
$350.00
In stock
25mg
$1,200.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

AZD-5597 is a potent CDK inhibitor with IC50 values of 2 nM for CDK1 and CDK2, respectively [1].

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 [1].

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 [1].

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% [1].

Reference:
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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt437.51
Cas No.924641-59-8
FormulaC23H28FN7O
Solubility≥15.65mg/mL in DMSO
Chemical Name(S)-(4-((5-fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methylamino)pyrrolidin-1-yl)methanone
SDFDownload SDF
Canonical SMILESCC(N1C(C)=NC=C1C2=NC(NC3=CC=C(C(N4CC[[email protected]@](NC)([H])C4)=O)C=C3)=NC=C2F)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Quality Control

Chemical structure

AZD-5597