CDK2-IN-51
CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer.
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- CAS No.: 1443-10-3
- Formule: C18H16N4
- Masse moléculaire:288.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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CDK2 23.47 nM (IC50) |
CDK2 4.11 μM (Ki) |
CDK2-IN-51 (compound 6) (10-50 μM; 24-72 h) demonstrates significant antiproliferative activity against HCT-116 and HT-29 cells with no cytotoxicity to NCM-460D cells[1].
CDK2-IN-51 (40-50 μM; 48 h) induces pre-G1 phase arrest in HCT-116 and HT-29 cells without S-phase arrest[1].
CDK2-IN-51 (40-50 μM; 48-72 h) downregulates CDK2 protein targets involved in DNA replication process; Polα, MCM7, ORC2, and ORC4 in HCT-116 and HT-29 cells, and does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, HT-29, NCM-460D
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Concentration:10 μM, 20 μM, 40 μM, 50 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:At 72 h, exhibited significant antiproliferative effects on HCT-116 and HT-29 cells, with IC50 values of 46.41 μM and 61.47 μM, respectively, and showed no cytotoxicity on NCM-460D cells, with an IC50 value of >100 μM.
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Cell Line:HCT-116, HT-29
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Concentration:40 μM, 50 μM
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Incubation Time:48 h
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Result:Caused a significant increase in the pre-G1 phase population in both HCT-116 and HT-29 cells, indicating cell death, and no S-phase arrest was observed, suggesting that the compound did not induce apoptosis.
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Cell Line:HCT-116, HT-29
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Concentration:40 μM, 50 μM
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Incubation Time:48 h, 72 h
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Result:Reduced the expression of CDK2 targets, MCM7, ORC2, and ORC4 proteins.
Reduced Polα levels.
Chemical Information
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CAS No. 1443-10-3
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Masse moléculaire 288.35
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Formule C18H16N4
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SMILES
CC1=NC2=NN3C(C)=CC(C)=NC3=C2C(C4=CC=CC=C4)=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)
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