1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. Chk1-IN-5

Chk1-IN-5 

Cat. No.: HY-131446
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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.

For research use only. We do not sell to patients.

Chk1-IN-5 Chemical Structure

Chk1-IN-5 Chemical Structure

CAS No. : 2120398-39-0

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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].

IC50 & Target[1]

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).
Molecular Weight

383.38

Formula

C₁₈H₁₈FN₇O₂

CAS No.

2120398-39-0

SMILES

N#CC1=NC=C(NC2=NNC(C3=C(OC)C=C(F)C=C3OCCCN)=C2)N=C1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Chk1-IN-5Checkpoint Kinase (Chk)HT-29colonChk1phosphorylationLoVoInhibitorinhibitorinhibit

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