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ChemicalBook--->CAS DataBase List--->924641-59-8

924641-59-8

924641-59-8 Structure

924641-59-8 Structure
IdentificationBack 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 PropertiesBack 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
Spectrum DetailBack Directory
[Spectrum Detail]

[4-[[5-Fluoro-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-2-pyrimidinyl]amino]phenyl][(3S)-3-(methylamino)-1-pyrrolidinyl]Methanone(924641-59-8)1HNMR
Hazard InformationBack 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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