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AZD-5597 Potent CDK inhibitor

Catalog No.B5926
Size Price Stock Qty
10mM (in 1mL DMSO)
$490.00
In stock
5mg
$350.00
In stock
25mg
$1,200.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AZD-5597

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Chemical Properties

Cas No. 924641-59-8 SDF Download SDF
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
Canonical SMILES CC(N1C(C)=NC=C1C2=NC(NC3=CC=C(C(N4CC[[email protected]@](NC)([H])C4)=O)C=C3)=NC=C2F)C
Formula C23H28FN7O M.Wt 437.51
Solubility >15.65mg/mL in DMSO Storage Store at -20°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.

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.