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Results for "

Nucleotide exchange assay

" in MedChemExpress (MCE) Product Catalog:

5

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3

Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-134813
    MRTX1133
    45+ Cited Publications

    		 Ras Cancer
    MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
    MRTX1133
  • HY-179414
    KRAS G12D-IN-34

    		Ras Cancer
    KRAS G12D-IN-34 (Compound 13) is a KRAS (G12D) inhibitor with IC50 values for KRAS (G12D) and KRAS (WT) of 1.05 nM and 1.59 μM respectively. KRAS G12D-IN-34 can be used for research on non-small cell lung cancer .
    KRAS G12D-IN-34
  • HY-162446
    pan-KRAS-IN-13

    		Ras Cancer
    pan-KRAS-IN-13 (compound 2) is a potent inhibitor of KRAS, with IC50s of 2.75 nM and 2.89 nM for G12D and G12V, respectively
    pan-KRAS-IN-13
  • HY-175326
    SOS1-IN-21

    		SOS1 Cancer
    SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
    SOS1-IN-21
  • HY-180920
    KRAS G12D-IN-36

    		Ras ERK Cancer
    KRAS G12D-IN-36 (Compound 53a) is a highly selective and orally active KRAS-G12D inhibitor with an IC50 of 1.63 nM. KRAS G12D-IN-36 effectively inhibits p-ERK with an IC50 of 8.4 nM. KRAS G12D-IN-36 shows potent anti-proliferative activity against AsPC-1 cells. KRAS G12D-IN-36 can be used for research on pancreatic cancer .
    KRAS G12D-IN-36

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