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

R406 free base 

Cat. No.: HY-11108 Purity: 99.25%
Handling Instructions

R406 free base is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.

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

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 672 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1164 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of R406 free base:

Top Publications Citing Use of Products

    R406 free base 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 free base 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.
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    Description

    R406 free base is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. IC50 value: 41 nM [1] Target: Syk in vitro: R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling. R406 inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 binds to the ATP binding pocket of Syk and inhibits its kinase activity as an ATP-competitive inhibitor with Ki of 30 nM. R406 blocks Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and Bcr-mediated activation of B lymphocytes [1]. R406 significantly induces chronic lymphocytic leukemia (CLL) cell apoptosis in nurselike cells cocultures and blocks CCL3 and CCL4 secretion by CLL cells in response to B-cell antigen receptor (Bcr) triggering [2]. R406 is a potent inhibitor of platelet signaling and functions initiated by FcγRIIA cross-linking by specific antibodies or by sera from HIT patients [3]. in vivo: R406 reduces cutaneous reverse passive Arthus reaction by approximately 86% at 5 mg/kg in prophylactic treated mice. R406 also shows efficacy in inhibiting paw inflammation in antibody-induced arthritis mouse models [1]. R406 does not adversely affect macrophage or neutrophil function in innate immune responses and has minimal functional immunotoxicity notwithstanding its lymphocytopenic effect [4].

    Molecular Weight

    470.45

    Formula

    C₂₂H₂₃FN₆O₅

    CAS No.

    841290-80-0

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 10 mg/mL (21.26 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2126 mL 1.0628 mL 2.1256 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References

    Purity: 99.25%

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    Product Name:
    R406 free base
    Cat. No.:
    HY-11108
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