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R406 free base

37 Cited Publications
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Based on 37 publication(s) in Google Scholar

R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).

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  • 純度: 99.07%
  • CAS 番号: 841290-80-0
  • 分子式: C22H23FN6O5
  • 分子量:470.45
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • R406 free base Chemical Structure
    R406 free base 構造式
  • Experimental Validation Results for R406 free base
  • Experimental Validation Results for R406 free base
  • Experimental Validation Results for R406 free base
  • Experimental Validation Results for R406 free base
  • Experimental Validation Results for R406 free base
CAS 番号: 841290-80-0
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Cell Migration/Invasion AssayWBFlow CytometryIP
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  • R406 free base Chemical Structure
    R406 free base Chemical Structure
    1/16
  • 1/16

    R406 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Apr 19;13(1):2136. [Abstract]

    Customer Validation
     Comparison of pharmacological inhibitors with the corresponding guides of positive and negative controls for BCR-controlled adhesion. Top plots: Namalwa cells pretreated with 100 nM ibrutinib (BTK inhibitor), 1 μM R406 (Fostamatinib, SYK inhibitor, 1 ), 100 nM wortmannin (pan-PI3K inhibitor), 50 μM PD-98059 (MEK1/2 inhibitor), 2.5 μM MK-2206 (AKT1/2/3 inhibitor), or DMSO control, were stimulated with αIgM or PMA, and allowed to adhere to fibronectin-coated surfaces. Bar graphs are presented as normalized mean + SEM (100% = untreated αIgM-stimulated cells). Bottom plots: MA plots of αIgM-induced adhesion relative to PMA-induced adhesion; the guides of the corresponding genes targeted by the inhibitors of the top plots are highlighted.

  • 1/16

    R406 free base purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2022 Nov 8;11(1):88. [Abstract]

    Customer Validation
     R406 (1-2 μM; 18-24 h) markedly inhibited C. tropicalis-induced PKM2 Tyr105 phosphorylation and PKM2 nuclear translocation in MDSCs by suppressing Syk.

  • 1/16

    R406 free base purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 May 24;11(15):7308-7321. [Abstract]

    Customer Validation
     The induction of IL-21 secretion by CBP-12-OVA was inhibited by R406, an inhibitor of Syk phosphorylation. FL-DCs were incubated with 2.5 µM R406 for 1 h, and then cultured with 100 µg/mL of the indicated peptides for 6 h at 37 °C. IL-21 positive frequency was determined by ICS assay.

  • 1/16

    R406 free base purchased from MedChemExpress. Usage Cited in: Cell. 2018 Oct 4;175(2):442-457.e23. [Abstract]

    Customer Validation
     Syk inhibitors (R406 (5 μM) and Piceatannol) are added during the induction of trastuzumab-dependent BT-474 phagocytosis. The binding of the phagosome marker Rab7 to AIM2 in macrophages are evaluated by co-immunoprecipitation.

  • 1/16

    R406 free base purchased from MedChemExpress. Usage Cited in: J Pharmacol Sci. 2017 May;134(1):29-36. [Abstract]

    Customer Validation
     The effects of R406 treatment on the phosphorylation of 3BP2 and p38MAPK in white blood cells from the spleens of NZB/W F1 mice. (A) The phosphorylation of the 3BP2 and (B) the phosphorylation of p38MAPK in the renal cortex of control and R406-treated mice.

  • R406 free base