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

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).

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

R406 free base Chemical Structure

R406 free base Chemical Structure

CAS No. : 841290-80-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 83 In-stock
Solution
10 mM * 1 mL in DMSO USD 83 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 80 In-stock
10 mg USD 130 In-stock
50 mg USD 430 In-stock
100 mg USD 680 In-stock
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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of R406 free base:

Top Publications Citing Use of Products

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

    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.

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

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1]. R406 free base 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].

    MedChemExpress (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].

    MedChemExpress (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

    470.45

    Formula

    C22H23FN6O5

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 25 mg/mL (53.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1256 mL 10.6281 mL 21.2562 mL
    5 mM 0.4251 mL 2.1256 mL 4.2512 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: 2.5 mg/mL (5.31 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.80%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1256 mL 10.6281 mL 21.2562 mL 53.1406 mL
    5 mM 0.4251 mL 2.1256 mL 4.2512 mL 10.6281 mL
    10 mM 0.2126 mL 1.0628 mL 2.1256 mL 5.3141 mL
    15 mM 0.1417 mL 0.7085 mL 1.4171 mL 3.5427 mL
    20 mM 0.1063 mL 0.5314 mL 1.0628 mL 2.6570 mL
    25 mM 0.0850 mL 0.4251 mL 0.8502 mL 2.1256 mL
    30 mM 0.0709 mL 0.3543 mL 0.7085 mL 1.7714 mL
    40 mM 0.0531 mL 0.2657 mL 0.5314 mL 1.3285 mL
    50 mM 0.0425 mL 0.2126 mL 0.4251 mL 1.0628 mL
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    R406 free base Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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