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.

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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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Chk1-IN-5

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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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (130.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6084 mL 13.0419 mL 26.0838 mL
5 mM 0.5217 mL 2.6084 mL 5.2168 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6084 mL 13.0419 mL 26.0838 mL 65.2095 mL
5 mM 0.5217 mL 2.6084 mL 5.2168 mL 13.0419 mL
10 mM 0.2608 mL 1.3042 mL 2.6084 mL 6.5209 mL
15 mM 0.1739 mL 0.8695 mL 1.7389 mL 4.3473 mL
20 mM 0.1304 mL 0.6521 mL 1.3042 mL 3.2605 mL
25 mM 0.1043 mL 0.5217 mL 1.0434 mL 2.6084 mL
30 mM 0.0869 mL 0.4347 mL 0.8695 mL 2.1736 mL
40 mM 0.0652 mL 0.3260 mL 0.6521 mL 1.6302 mL
50 mM 0.0522 mL 0.2608 mL 0.5217 mL 1.3042 mL
60 mM 0.0435 mL 0.2174 mL 0.4347 mL 1.0868 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8151 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6521 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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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