A dual inhibitor of Aurora kinase (Kds = 7.5 and 48 nM for Aurora A and B

CCT241736 – 10 mg

Brand:
Cayman
CAS:
1402709-93-6
Storage:
-20
UN-No:
Non-Hazardous - /

CCT241736 is a dual inhibitor of Aurora kinases (Kds = 7.5 and 48 nM for Aurora A and B, respectively) and FLT3 (Kds = 6.2, 38, and 14 nM for wild-type, FLT3ITD, and FLT3D835Y, respectively).{27919} It also inhibits the activity of 22 additional kinases by greater than 90% in a panel of 386 nonmutant kinases at 1 µM. CCT241736 inhibits cell growth of SW620, HCT116, MOLM-13, and MV4-11 cancer cells (GI50s = 1, 0.3, 0.1, and 0.3 µM, respectively). Oral administration of CCT241736 (50 mg/kg twice per day) reduces tumor growth by 58% in an MV4-11 mouse xenograft model.  

 

Available on backorder

Add to quotes
SKU: 26185 - 10 mg Category:

Description

A dual inhibitor of Aurora kinase (Kds = 7.5 and 48 nM for Aurora A and B, respectively) and FLT3 (Kds = 6.2, 38, and 14 nM for wild-type, FLT3ITD, and FLT3D835Y, respectively); inhibits the activity of 22 additional kinases by >90% in a panel of 386 nonmutant kinases at 1 µM; inhibits cell growth of SW620, HCT116, MOLM-13, and MV4-11 cancer cells (GI50s = 1, 0.3, 0.1, and 0.3 µM, respectively); oral administration reduces tumor growth by 58% in an MV4-11 mouse xenograft model at 50 mg/kg

Formal name: 6-chloro-7-[4-[(4-chlorophenyl)methyl]-1-piperazinyl]-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine

Synonyms: 

Molecular weight: 456.4

CAS: 1402709-93-6

Purity: ≥90%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Aurora Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cell Biology|Cell Signaling

Related products

  • 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
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 1 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 1 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 – 250 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 - 250 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