2120398-39-0

2120398-39-0 structure
2120398-39-0 structure
  • Name: Chk1-IN-5
  • Chemical Name: Chk1-IN-5
  • CAS Number: 2120398-39-0
  • Molecular Formula: C18H18FN7O2
  • Molecular Weight: 383.38
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Checkpoint Kinase (Chk)
  • Create Date: 2020-10-17 21:19:55
  • Modify Date: 2024-01-10 13:18:20
  • 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].

Name Chk1-IN-5
Description 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].
Related Catalog
Target

Chk1

In Vitro Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells[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. 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).
References

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

Molecular Formula C18H18FN7O2
Molecular Weight 383.38
Hazard Codes Xi
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