An allosteric inhibitor of FGFR2; inhibits FGF2-induced phosphorylation of FRS2α in KATO III cells (IC50 = 10 nM); inhibits the growth of SKOV3 and Hs 578T cells (GI50s = 370 and 210 nM

Alofanib – 50 mg

Brand:
Cayman
CAS:
1612888-66-0
Storage:
-20
UN-No:
Non-Hazardous - /

Alofanib is an allosteric inhibitor of FGFR2.{58160,58161} It inhibits FGF2-induced phosphorylation of FGFR substrate 2 (FRS2α) in KATO III gastric carcinoma cells (IC50 = 50s = 370 and 210 nM, respectively). It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) induced by basic FGF (bFGF; IC50 = 11 nM) and tube formation of SVEC4-10 endothelial cells when used at a concentration of 50 nM.{58160} It also inhibits migration of SVEC4-10 cells in a wound healing assay. Alofanib (50 mg/kg) decreases the number of microvessels in tumor tissue by 50% in a SKOV3 ovarian serous carcinoma mouse model. It reduces tumor growth in mouse xenograft models when administered at a dose of 30 mg/kg per day, and the degree of tumor volume reduction positively correlates with the expression level of FGFR2{58161}  

 

Available on backorder

Add to quotes
SKU: 31754 - 50 mg Category:

Description

An allosteric inhibitor of FGFR2; inhibits FGF2-induced phosphorylation of FRS2α in KATO III cells (IC50 = 10 nM); inhibits the growth of SKOV3 and Hs 578T cells (GI50s = 370 and 210 nM, respectively); inhibits bFGF-induced HUVEC proliferation (IC50 = 11 nM); inhibits SVEC4-10 cell tube formation at 50 nM; decreases the number of tumor microvessels by 50% in a SKOV3 ovarian serous carcinoma mouse model; reduces tumor growth in mouse xenograft models at 30 mg/kg per day

Formal name: 3-[[[4-methyl-2-nitro-5-(3-pyridinyl)phenyl]amino]sulfonyl]-benzoic acid

Synonyms:  RPT835

Molecular weight: 413.4

CAS: 1612888-66-0

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 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 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 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 – 50 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 - 50 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