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

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.

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Chk1-IN-5 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Chk1-IN-5
Cat. No.:
HY-131446
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