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.
For research use only. We do not sell to patients.
- CAS No.: 2120398-41-4
- Formula: C18H18BrN7O2
- Molecular Weight:444.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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CAS No. 2120398-41-4
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Molecular Weight 444.29
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHK1-IN-4 Related Classifications
HY-128766 Related Classifications
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