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% .

Product information

CAS Number: 924641-59-8

Molecular Weight: 437.51

Formula: C23H28FN7O

Chemical Name: 5-fluoro-4-[2-methyl-1-(propan-2-yl)-1H-imidazol-5-yl]-N-{4-[(3S)-3-(methylamino)pyrrolidine-1-carbonyl]phenyl}pyrimidin-2-amine

Smiles: CC1=NC=C(C2=NC(NC3C=CC(=CC=3)C(=O)N3CC[C@@H](C3)NC)=NC=C2F)N1C(C)C

InChiKey: NTSDIJMNXYJJNG-SFHVURJKSA-N

InChi: InChI=1S/C23H28FN7O/c1-14(2)31-15(3)26-12-20(31)21-19(24)11-27-23(29-21)28-17-7-5-16(6-8-17)22(32)30-10-9-18(13-30)25-4/h5-8,11-12,14,18,25H,9-10,13H2,1-4H3,(H,27,28,29)/t18-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.