| Identification | Back Directory | [Name]
5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile | [CAS]
2120398-39-0 | [Synonyms]
Chk1-IN-5
5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
2-Pyrazinecarbonitrile, 5-[[5-[2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]- | [Molecular Formula]
C18H18FN7O2 | [MDL Number]
MFCD34470748 | [MOL File]
2120398-39-0.mol | [Molecular Weight]
383.38 |
| Hazard Information | Back Directory | [Uses]
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model[1]. | [in vivo]
Chk1-IN-5 (compound 3; 40 mg/kg; IV; twice a week for 21 days) inhibits tumor growth in Baib/c nude mice with HT-29 colon cancer cells[1].
Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr?kg; Vss=6.4 L/kg; AUC=4531 ng/ml?h)[1].
| Animal Model: | Baib/c nude mice with HT-29 colon cancer cells[1] | | Dosage: | 40 mg/kg | | Administration: | IV; twice a week for 21 days | | Result: | Inhibited tumor growth.
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| Animal Model: | Male SD rats (280-350 g)[1] | | Dosage: | 10 mg/kg | | Administration: | Via tail vein intravenous injection | | Result: | Displayed a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr?kg; Vss=6.4 L/kg; AUC=4531 ng/ml?h).
|
| [IC 50]
Chk1 | [References]
[1] Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1. |
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