Identification | Back Directory | [Name]
[4-[[5-Fluoro-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-2-pyrimidinyl]amino]phenyl][(3S)-3-(methylamino)-1-pyrrolidinyl]Methanone | [CAS]
924641-59-8 | [Synonyms]
CS-1058 AZD 5597 pyrimidin-2-yl) (3-(methylamino) AZD 5597; AZD5597 -(4-((5-Fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl) (S)-(4-((5-Fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(met (S)-(4-((5-Fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methyl (S)-(4-((5-Fluoro-4-(1-isopropyl-2-Methyl-1H-iMidazol-5-yl)pyriMidin-2-yl)aMino)phenyl)(3-(MethylaMino)pyrrolidin-1-yl)Methanone 4-[[5-Fluoro-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-ly]-2-pyrimidinyl]amino]phenyl][(3S)-3-(methylamino)-1-pyrrolidinyl]methanone [4-[[5-Fluoro-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-2-pyrimidinyl]amino]phenyl][(3S)-3-(methylamino)-1-pyrrolidinyl]Methanone Methanone, [4-[[5-fluoro-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-2-pyrimidinyl]amino]phenyl][(3S)-3-(methylamino)-1-pyrrolidinyl]- | [Molecular Formula]
C23H28FN7O | [MDL Number]
MFCD13184818 | [MOL File]
924641-59-8.mol | [Molecular Weight]
437.51 |
Chemical Properties | Back Directory | [Boiling point ]
679.0±65.0 °C(Predicted) | [density ]
1.32 | [storage temp. ]
2-8°C(protect from light) | [solubility ]
≥1.82 mg/mL in H2O with ultrasonic; ≥12.7 mg/mL in EtOH; ≥15.65 mg/mL in DMSO | [form ]
solid | [pka]
9.66±0.20(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
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. |
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Cckinase, Inc.
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+1 (732)236-3202 |
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www.cckinase.com |
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