A potent

GNF-5837 – 1 mg

Brand:
Cayman
CAS:
1033769-28-6
Storage:
-20
UN-No:
Non-Hazardous - /

Tropomyosin-related kinases (Trks) are receptor tyrosine kinases activated by peptides, including neurotrophins. They have prominent roles in the development of central and peripheral nervous systems, vascular cell survival, and cancer.{30894} Rearrangement of genes for Trks with the transcription factor Tel, producing Tel-Trk fusion proteins, are associated with various types of cancer.{30895,30893} GNF-5837 is a potent, bioavailable pan-Trk inhibitor that blocks the proliferation of cells expressing Tel-TrkA, Tel-TrkB, and Tel-TrkC (IC50s = 7, 9, and 11 nM, respectively).{30893} It less effectively inhibits c-Kit and PDGFRβ (IC50s = 0.91 and 0.87 µM, respectively), while requiring micromolar concentrations to inhibit an array of other receptor and non-receptor tyrosine kinases. GNF-5837 inhibits the growth of Ba/F3 and rat intestinal epithelial (RIE) cells expressing both TrkA and nerve growth factor (NGF) with IC50 values of 42 and 17 nM, respectively, but does not have anti-proliferative activity of parental cells at concentrations up to 10 µM.{30893} GNF-5837 displays good bioavailability in mice and rats when given intravenously but not orally.{30893} It induces regression of tumor xenografts derived from RIE cells expressing both TrkA and NGF.{30893}  

 

Add to quotes
SKU: - Category:

Description

A potent, bioavailable pan-Trk inhibitor that blocks the proliferation of cells expressing TEL-TrkA, TEL-TrkB, and TEL-TrkC (IC50s = 7, 9, and 11 nM, respectively); inhibits the growth of Ba/F3 and RIE cells expressing both TrkA and NGF with IC50 values of 42 and 17 nM, respectively

Formal name: N-[3-[[2,3-dihydro-2-oxo-3-(1H-pyrrol-2-ylmethylene)-1H-indol-6-yl]amino]-4-methylphenyl]-N’-[2-fluoro-5-(trifluoromethyl)phenyl]-urea

Synonyms: 

Molecular weight: 535.5

CAS: 1033769-28-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 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 - 100 mg

    Available on backorder

    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 – 10 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 - 10 mg

    Available on backorder

    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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 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 - 10 µg

    Available on backorder

    Add to quotes
    View product page