An inhibitor of Src kinases (IC50s = 50 = 479 nM)

eCF506 – 10 mg

Brand:
Cayman
CAS:
1914078-41-3
Storage:
-20
UN-No:
Non-Hazardous - /

eCF506 is an inhibitor of Src kinases (IC50s = 50 = 479 nM), as well as KIT, mTOR, PDGFRα, and RET (IC50s = >100 µM for all). eCF506 completely inhibits phosphorylation of Src and FAK, a downstream Src substrate, in MCF-7 and MDA-MB-231 cells when used at a concentration of 100 nM. It also inhibits proliferation of MCF-7 cells (EC50 = 9 nM) and induces apoptosis. eCF506 (50 mg/kg per day) reduces levels of activated Src kinase in tumor tissue in an HCT116 mouse xenograft model.  

 

Available on backorder

Add to quotes
SKU: 19959 - Category:

Description

An inhibitor of Src kinases (IC50s = 50 = 479 nM), as well as KIT, mTOR, PDGFRα, and RET (IC50s = >100 µM for all); completely inhibits Src and FAK phosphorylation at 100 nM; inhibits proliferation of MCF-7 cells (EC50 = 9 nM); reduces levels of activated Src kinase in tumor tissue in an HCT116 mouse xenograft model at 50 mg/kg per day

Formal name: N-[4-[4-amino-1-[2-[4-(dimethylamino)-1-piperidinyl]ethyl]-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]-carbamic acid, 1,1-dimethylethyl ester

Synonyms: 

Molecular weight: 510.6

CAS: 1914078-41-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis

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

    (R)-Roscovitine – 500 µg

    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 - 500 µg

    Available on backorder

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

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 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 - 25 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