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

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
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 183 In-stock
Solution
10 mM * 1 mL in DMSO USD 183 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 198 In-stock
50 mg USD 792 In-stock
100 mg USD 1188 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of R406:

Top Publications Citing Use of Products

    R406 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 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 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].

    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

    628.63

    Formula

    C28H29FN6O8S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 61 mg/mL (97.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (3.98 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (3.98 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5908 mL 7.9538 mL 15.9076 mL 39.7690 mL
    5 mM 0.3182 mL 1.5908 mL 3.1815 mL 7.9538 mL
    10 mM 0.1591 mL 0.7954 mL 1.5908 mL 3.9769 mL
    15 mM 0.1061 mL 0.5303 mL 1.0605 mL 2.6513 mL
    20 mM 0.0795 mL 0.3977 mL 0.7954 mL 1.9885 mL
    25 mM 0.0636 mL 0.3182 mL 0.6363 mL 1.5908 mL
    30 mM 0.0530 mL 0.2651 mL 0.5303 mL 1.3256 mL
    40 mM 0.0398 mL 0.1988 mL 0.3977 mL 0.9942 mL
    50 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7954 mL
    60 mM 0.0265 mL 0.1326 mL 0.2651 mL 0.6628 mL
    80 mM 0.0199 mL 0.0994 mL 0.1988 mL 0.4971 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    R406 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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    R406
    Cat. No.:
    HY-12067
    Quantity:
    MCE Japan Authorized Agent: