CHK1-IN-4
CHK1-IN-4 is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 ≤ 1 nM. The IC50 value of CHK1-IN-4 against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 can be used for the research of colon cancer and breast cancer.
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- CAS No.: 2120398-41-4
- Formule: C18H18BrN7O2
- Masse moléculaire:444.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
Chk1 ≤ 1 nM (IC50) |
In Vitro
CHK1-IN-4 (Compound 3) inhibits the proliferation of HT-29 colon cancer cells and MDA-MB-231 breast cancer cells, with IC50 values ranging from 10-50 nM and 50-100 nM, respectively[1].
CHK1-IN-4 (0.4-33.3 nM; 16.5-27 h) potently inhibits SN-38 (HY-13704)-induced Chk1S296 phosphorylation in HT-29 colon cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | AUC0-t | AUC0-inf | MRT | Vd | Vss | CL |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 3.8 h | 4531 ng/mL·h | 4637 ng/mL·h | 2.8 h | 12.3 L/kg | 6.4 L/kg | 2.3 L/h/kg |
In Vivo
CHK1-IN-4 (10-40 mg/kg; intravenous injection; twice weekly) exhibits dose-dependent tumor growth inhibition in the LoVo colon cancer xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 2120398-41-4
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Masse moléculaire 444.29
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Formule C18H18BrN7O2
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SMILES
N#CC1=NC=C(NC2=NNC(C3=C(OC)C=C(Br)C=C3OCCCN)=C2)N=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)