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Results for "

Gatekeeper mutations

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Biochemical Assay Reagents

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-139590
    Zeteletinib

    BOS-172738; DS-5010

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
    Zeteletinib
  • HY-15814
    HG-7-85-01

    		Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
    HG-7-85-01
  • HY-W005118
    2-Amino-4-fluoropyridine

    4-Fluoropyridin-2-amine

    		 Drug Intermediate Cancer
    2-Amino-4-fluoropyridine (4-Fluoropyridin-2-amine) is a drug intermediate that can be used for the synthesis reversible-covalent FGFR4 inhibitors .
    2-Amino-4-fluoropyridine
  • HY-134301A
    8-ET-NAD+ sodium

    8-Ethylthio-NAD+ sodium

    		 PARP Cancer
    8-ET-NAD+ (sodium) is the derivative of NAD+. 8-ET-NAD+ (sodium) can be used in screening of PARP1 gatekeeper mutations. 8-ET-NAD+ (sodium) can be studied in research on cancer .
    8-ET-NAD+ sodium
  • HY-134300A
    8-DMA-NAD+ sodium

    8-Dimethylamino-NAD+ sodium

    		 Endogenous Metabolite Others
    8-DMA-NAD+ (sodium) (8-Dimethylamino-NAD+ (sodium)) is a derivative of the signaling molecule and enzyme cofactor NAD+ (HY-B0445). 8-DMA-NAD+ (sodium) can be used in the screening of analog-sensitive poly (ADP-ribose) polymerase 1 (PARP1) gatekeeper mutations .
    8-DMA-NAD+ sodium
  • HY-134305A
    8-MA-NAD+ sodium

    8-Methylamino-NAD+ sodium

    		 Endogenous Metabolite Others
    8-MA-NAD+ (sodium) (8-Methylamino-NAD+ (sodium)) is a derivative of the signaling molecule and enzyme cofactor NAD+ (HY-B0445). 8-MA-NAD+ (sodium) can be used in the screening of analog-sensitive poly (ADP-ribose) polymerase 1 (PARP1) gatekeeper mutations. 8-MA-NAD+ (sodium) can be used in the synthesis of cyclic ADP-ribose (cADPR) derivatives .
    8-MA-NAD+ sodium
  • HY-139590A
    Zeteletinib hemiadipate

    BOS-172738 hemiadipate; DS-5010 hemiadipate

    		 RET PDGFR Cancer
    Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
    Zeteletinib hemiadipate
  • HY-160478
    GNF-6

    		Bcr-Abl Cancer
    GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
    GNF-6
  • HY-E70717
    FGFR1 V561M Recombinant Human Active Protein Kinase

    		FGFR Cancer
    FGFR1 has been implicated in numerous cancer types including non-small cell lung cancer (NSCLC). FGFR1 is activated upon FGF binding to its extracellular domain, resulting in protein dimerization and transautophosphorylation of the intracellular tyrosine kinase domains. FGFR1 V561M gatekeeper mutation drives Fexagratinib (AZD4547) (HY-13330) resistance through STAT3 Activation and EMT. FGFR1 V561M Recombinant Human Active Protein Kinase is a recombinant FGFR1 V561M protein that can be used to study FGFR1 V561M-related functions .
    FGFR1 V561M Recombinant Human Active Protein Kinase

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