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.  

 

Available on backorder

Add to quotes
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

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 100 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 500 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page