1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Syk
    FLT3
    Apoptosis
  3. R406

R406 

Cat. No.: HY-12067 Purity: 96.67%
Handling Instructions

R406 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 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).

For research use only. We do not sell to patients.

R406 Chemical Structure

R406 Chemical Structure

CAS No. : 841290-81-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of R406:

Top Publications Citing Use of Products

    R406 purchased from MCE. Usage Cited in: J Pharmacol Sci. 2017 May;134(1):29-36.

    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 purchased from MCE. Usage Cited in: Cell. 2018 Oct 4;175(2):442-457.e23.

    Syk inhibitors (R406 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.
    • Biological Activity

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    • Customer Review

    Description

    R406 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 reduces immune complex-mediated inflammation[1]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].

    IC50 & Target

    Ki: 30 nM (Syk)[1]
    IC50: 41 nM (Syk)[1]
    FLT3[1]
    IC50: 63 nM (Lyn), 37 nM (Lck)[2]

    In Vitro

    R406 inhibits adenosine A3 receptor (IC50=0.081 µM), adenosine transporter (IC50=1.84 µM), and monoamine transporter (IC50=2.74 µM)[1].
    R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 µM, respectively[1].
    R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[1]

    Cell Line: Cultured human mast cells (CHMC)
    Concentration: 0.016, 0.08, 0.4, 2 µM
    Incubation Time: 40 minutes
    Result: Inhibited all other kinases tested at 5 to 100 fold less potency than Syk as judged by phosphorylation of target proteins.
    In Vivo

    R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female Balb/c mice (6-8 weeks) with CAIA[1]
    Dosage: 5 and 10 mg/kg
    Administration: Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
    Result: Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.
    Animal Model: Female C57BL/6 mice with arthritis[1]
    Dosage: 10 mg/kg
    Administration: Administered orally one hour before serum injection; b.i.d; for 13 days
    Result: Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.
    Molecular Weight

    628.63

    Formula

    C₂₈H₂₉FN₆O₈S

    CAS No.

    841290-81-1

    SMILES

    COC1=CC(NC2=NC(NC3=NC(N4)=C(C=C3)OC(C)(C)C4=O)=C(C=N2)F)=CC(OC)=C1OC.OS(C5=CC=CC=C5)(=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 61 mg/mL (97.04 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5908 mL 7.9538 mL 15.9076 mL
    5 mM 0.3182 mL 1.5908 mL 3.1815 mL
    10 mM 0.1591 mL 0.7954 mL 1.5908 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (3.98 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    R406R 406R-406SykFLT3ApoptosisSpleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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