A potent Chk1 inhibitor (IC50 = 8 nM); selective for Chk1 over FLT3

CCT244747 – 5 mg

Brand:
Cayman
CAS:
1404095-34-6
Storage:
-20
UN-No:
Non-Hazardous - /

CCT244747 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC50 = 8 nM).{41934} It is selective for Chk1 over FLT3, Chk2, and CDK1 (IC50s = 600, >10,000, and >10,000 nM, respectively) as well as a panel of 121 additional kinases at a concentration of 10 μM. CCT244747 reverses cell cycle arrest at the G2/M phase induced by etoposide (Item No. 12092) and SN-38 (Item No. 15632) in HT-29 cells and gemcitabine (Item Nos. 11690 | 9003096) in SW620 cells, indicating cellular G2 checkpoint abrogation. It potentiates the genotoxicity of SN-38, gemcitabine, and etoposide in HT-29, SW620, MiaPaCa-2, and Calu-6 cells with potentiation index (PI) values ranging from 1.9-8.5, 2.6-12.2, 5-16, and 1.4-5.6, respectively. In vivo, CCT244747 (75 mg/kg), in combination with irinotecan (Item No. 14180) or gemcitabine, increases the delay of tumor growth in SW620 and Calu-6 mouse xenograft models, respectively.  

 

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SKU: 25666 - 5 mg Category:

Description

A potent Chk1 inhibitor (IC50 = 8 nM); selective for Chk1 over FLT3, Chk2, and CDK1 (IC50s = 600, >10,000, and >10,000 nM, respectively) as well as a panel of 121 additional kinases at 10 μM; reverses cell cycle arrest at the G2/M phase induced by etoposide and SN-38 in HT-29 cells and gemcitabine in SW620 cells; potentiates the genotoxicity of SN-38, gemcitabine, and etoposide in HT-29, SW620, MiaPaCa-2, and Calu-6 cells; in combination with irinotecan or gemcitabine, increases the delay of tumor growth in SW620 and Calu-6 mouse xenograft models, respectively, at 75 mg/kg

Formal name: 3-[(1R)-2-(dimethylamino)-1-methylethoxy]-5-[[4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile

Synonyms: 

Molecular weight: 408.5

CAS: 1404095-34-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Signaling

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