R406

Catalog No.S2194

R406 Chemical Structure

Molecular Weight(MW): 628.63

R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.

Size Price Stock Quantity  
In DMSO USD 286 In stock
USD 120 In stock
USD 170 In stock
USD 270 In stock
USD 870 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

6 Customer Reviews

  • The patient's CLL cells were exposed to dabrafenib, vemurafenib, R406, or DMSO as control at the indicated concentrations, and the resulting Western blot and the RAS-GTP/tRAS ratios are shown. One of 3 independent experiments with similar results is shown.

    J Clin Invest 2014 124(11), 5074-84. R406 purchased from Selleck.

    Platelets (3 x 108/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).

    Blood 2014 122(4), 580-9. R406 purchased from Selleck.

  • (C) Z-138 and JEKO-1 cells were simultaneously  exposed  to sorafenib and R406  at  the  indicated doses, and cell viability was determined at 48 hours by annexin  V/PI  staining.  Bars represent the mean ± SD of 3 independent experiments. CI value is indicated for each combination. (D)  Primary MCL cells from 7 patients were simultaneously exposed to sorafenib and R406 at the indicated doses for 48 hours, and cell viability was determined as above. Bars represent the mean ± SEM of all the samples analyzed. CI value is indicated for each combination.

    Clin Cancer Res 2013 19, 586-597. R406 purchased from Selleck.

    NHEKs were treated with R406 (1 μM) for 1, 3, and 5 days. Then cells were collected for the protein analysis by Western blot.

    J Invest Dermatol, 2016, 136(1):192-201. R406 purchased from Selleck.

  • (M-CSF)-M2 macrophages were exposed to M860-IC (30 µg/ml) for 18 h in the presence of heparin or R406 (0, 1, 3 µM), mAbs against human CD14, CD16, CD32, CD64, or CLI-095 (5 µM). Isotype-matched irrelevant Abs as well as untreated (M-CSF)-M2 cells (M) were included as controls. TNFα in the culture supernatant was quantitated using ELISAs.

    Front Immunol, 2018, 9: 37. R406 purchased from Selleck.

    Neutrophils were pretreated or untreated with the indicated concentrations of R406 for 1 hr. The cells were stimulated with SAA (5 ug/ml) for 4 hr. The cells were harvested and analyzed for NLRP3 mRNA by RT-PCR. Three experiments were performed using different neutrophils and a representative result is shown.

    PLoS One 2014 9(5), e96703. R406 purchased from Selleck.

Purity & Quality Control

Choose Selective Syk Inhibitors

Biological Activity

Description R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.
Features Lead drug candidate for rheumatoid arthritis.
Targets
Flt3 [1]
(Cell-free assay)
Syk [1]
(Cell-free assay)
41 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
AMO-1 MnnmSpVv[3Srb36gRZN{[Xl? MnvoNUDPxE1? NVHBZ5d{O8LiaB?= NX\odHFNemWmdXPld{BucWe{YYTpc47DqA>? MXmyOlI2OTd4MR?=
U266 MnPkSpVv[3Srb36gRZN{[Xl? NVXsdlZOOSEQvF2= MWezxsBp M3rPepJm\HWlZYOgcYloemG2aX;uxsA> M4jSd|I3OjVzN{[x
Jeko-1 MoPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjsOFghcA>? M3zEcGlEPTB;NT6wOlgzPiEQvF2= NUnj[VkzOjV6M{W3OVU>
Mino M1:yc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoW3OFghcA>? NYK1O2RRUUN3ME21MlcxQDV2IN88US=> M2n6OVI2QDN3N{W1
Jeko-1 Mk\iRZBweHSxc3nzJGF{e2G7 NYnUWIoxPcLizszN MlTDNlQhcA>? M4ntSYlv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= M3zjTFI2QDN3N{W1
primary MCL NUHBOFI1SXCxcITvd4l{KEG|c3H5 Mn7JNkDDvU1? MWqyOEBp MkHObY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= MmPWNlU{QDh|N{O=
PBMCs MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWPMeHNFOC13MDFOwG0> MY[yOEBp MnP5SG1UVw>? NWHWdFl5cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NFznVXMzPTF{N{i2Ni=>
PBMCs MVLGeY5kfGmxbjDBd5NigQ>? NYPqOnl{PSEQvF2= M37KPVEhcA>? NVjMTnN{TE2VTx?= Mmj4[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> NETaNmozPTF{N{i2Ni=>
CFSE-CD4+ T  NGf1OIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnpNE4xPjJ3LUGg{txO NHTkU4U1KGR? NFTO[mNjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= MWmyOFY4QTl6Mh?=
CFSE-CD11b+ NYDmdI0{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7RZVUxNjB4MkWtNUDPxE1? M3XuNlgh\A>? NUjUO|Y{[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= MYSyOFY4QTl6Mh?=
HMECs NFO4bopHfW6ldHnvckBCe3OjeR?= Ml3nNE0yOCEQvF2= NGjXe4wzOCCvaX6= NImwfIlqdmirYnn0d{BXTUeILYP0bY12dGG2ZXSgdoVt\WG|ZTDv[kBPVw>? NGKyTGQzPDN{OUW0OC=>
AB5 NVrRW4xLSXCxcITvd4l{KEG|c3H5 MYCwMVIvPSEQvF2= MlnPOFghcA>? M3\qc2ROW09? MnPVbY5lfWOnczDhdI9xfG:|aYO= NIm1NogzOzN7OEmxNS=>
JB7 NXr0eXNOSXCxcITvd4l{KEG|c3H5 M3PJTFAuOi53IN88US=> NVrMNWx2PDhiaB?= NV3EToVSTE2VTx?= NVfhUHZHcW6mdXPld{BieG:ydH;zbZM> MViyN|M6QDlzMR?=
AB5 NYXvRlVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUewMVIvPSEQvF2= NVO2OY9LPDhiaB?= NIj6bVFFVVOR MlqxbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NEf1do8zOzN7OEmxNS=>
JB7 M2nOe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGwMVIvPSEQvF2= NVqzeoNbPDhiaB?= MmjsSG1UVw>? M{\ueolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NWS4TlJFOjN|OUi5NVE>
RL MYrGeY5kfGmxbjDBd5NigQ>? NIi0O4wzNjVxNTFOwG0> MXmyOE81QCCq NYXIVo9ETE2VTx?= M4i4fYlv\HWlZYOgZUBxd3SnboSg[IVkemWjc3WgbY4hVU2SLUmgcXJPSSCneIDy[ZN{cW:w Ml;QNlE6OjZ7NkW=
RL MmXaSpVv[3Srb36gRZN{[Xl? MmX3NU8zNjVizszN M1HNW|I1KGh? NVXnUGtSTE2VTx?= M1j2O5Jm\HWlZYOgeIhmKGGldHn2ZZRqd25ib3[gRYt1KGGwZDDwO|BUPkt? NGKxdZozOTl{Nkm2OS=>
platelet  NXe3Tm5lTnWwY4Tpc44hSXO|YYm= Ml7xNeKh|ryv NWTJd|BlPSCvaX6= NFzOOZhqdmirYnn0d{BH[87|UlnJRU1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdg>? MUmyNVg1QDZ7NB?=
platelet  MVXGeY5kfGmxbjDBd5NigQ>? MXWwMlA2NzFxMj61JO69VQ>? MoLWOUBucW5? M1frOIlvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC NXfqVIZDOjF6NEi2PVQ>
DoHH2 MYrBdI9xfG:|aYOgRZN{[Xl? NHTCcWIxNzNxMUCg{txO NEHsfm41QCCq NXj6fmdlcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MkTsNlA5PzV2MEi=
Jeko-1  MXXBdI9xfG:|aYOgRZN{[Xl? MoXpNE8{NzFyIN88US=> NYrWSGRqPDhiaB?= MXvpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? NUK1OHJ[OjB6N{W0NFg>
Raji  NXrGXVlxSXCxcITvd4l{KEG|c3H5 NEjRRXAxNzNxMUCg{txO M{DFfFQ5KGh? MnrybY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? MlLQNlA5PzV2MEi=
DHL4 MknURZBweHSxc3nzJGF{e2G7 NU[2engxOC9zL{Sg{txO MV25OkBp NGjBR|NqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4HaZ|E5ODB4Nkm2
LY7 NITzNnNCeG:ydH;zbZMhSXO|YYm= NHvse4kxNzFxNDFOwG0> MYm5OkBp M2DJb4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1P2cFE5ODB4Nkm2
LY3 NYHOZoJsSXCxcITvd4l{KEG|c3H5 M3nENlAwOS92IN88US=> MXS5OkBp MnXpbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MnrBNVgxODZ4OU[=
DHL6 NHi0WYtCeG:ydH;zbZMhSXO|YYm= NFfrSlAxNzFxNDFOwG0> MW[5OkBp NUS0TYtncW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NEWwdmkyQDByNk[5Oi=>
LY10 MUHBdI9xfG:|aYOgRZN{[Xl? Mm[1NE8yNzRizszN MYK5OkBp M{DNO4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MljpNVgxODZ4OU[=
DHL10 NFfRZnZCeG:ydH;zbZMhSXO|YYm= NEKycIkxNzFxNDFOwG0> NV3n[|J4QTZiaB?= NX;TWnc5cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MnLtNVgxODZ4OU[=
Wsu-NHL M4L4PGFxd3C2b4Ppd{BCe3OjeR?= M{G4b|AwOS92IN88US=> NUfST|RMQTZiaB?= NYPZdJhPcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NHrEPZMyQDByNk[5Oi=>
LY18 NXLuZ5ZuSXCxcITvd4l{KEG|c3H5 MmfWNE8yNzRizszN MoftPVYhcA>? NHu1fpVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFj1N5IyQDByNk[5Oi=>
LY1 M{Tr[2Fxd3C2b4Ppd{BCe3OjeR?= NHTVUnUxNzFxNDFOwG0> Ml7kPVYhcA>? M3Xy[4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M{fZOFE5ODB4Nkm2
DHL8 NVHxWVh4SXCxcITvd4l{KEG|c3H5 NEW3N2QxNzFxNDFOwG0> Mn65PVYhcA>? MoHMbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NWjqXWdEOThyME[2PVY>
DHL4 NIXpWm1CeG:ydH;zbZMhSXO|YYm= NULzboFbPCEQvF2= MUC5OkBp NF3iS3VqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NWnv[mN3OThyME[2PVY>
DHL6 MWPBdI9xfG:|aYOgRZN{[Xl? NEnMem41KM7:TR?= MlvRPVYhcA>? NF\hd|lqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NH7mU|cyQDByNk[5Oi=>
LY3 MlPHRZBweHSxc3nzJGF{e2G7 M2jURlQh|ryP NV;wfWVRQTZiaB?= Mn:4bY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MnTYNVgxODZ4OU[=
LY7 NFHPUGVCeG:ydH;zbZMhSXO|YYm= MWO0JO69VQ>? Mnf6PVYhcA>? MoHrbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> Mm\iNVgxODZ4OU[=
DHL4 NYfqNnBKTnWwY4Tpc44hSXO|YYm= MUC0JO69VQ>? M2L3OFE3KGh? M2\OUolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M1n4dFE5ODB4Nkm2
LY7 MV;GeY5kfGmxbjDBd5NigQ>? M3S5OlQh|ryP NV;t[4ZvOTZiaB?= M1LWb4lvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MVSxPFAxPjZ7Nh?=
LY3 MVfGeY5kfGmxbjDBd5NigQ>? NFLzOJo1KM7:TR?= M4PKPVE3KGh? M3;vXolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MWOxPFAxPjZ7Nh?=
DHL6 NUG3bY1CTnWwY4Tpc44hSXO|YYm= Ml\vOEDPxE1? NH20[pcyPiCq NGTCXYtqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MYmxPFAxPjZ7Nh?=
LY10 MX7GeY5kfGmxbjDBd5NigQ>? NXX4cZR{PCEQvF2= NHe1UJQyPiCq MnPGbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NXH2cG8yOThyME[2PVY>
Wsu-NHL NFfkfm9HfW6ldHnvckBCe3OjeR?= NEfQN4w1KM7:TR?= NHTuOG8yPiCq MnOxbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MnjVNVgxODZ4OU[=
LY18 MUjGeY5kfGmxbjDBd5NigQ>? M2rLTVQh|ryP NUfydJVYOTZiaB?= MnrlbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MnHJNVgxODZ4OU[=

... Click to View More Cell Line Experimental Data

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]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Arthritis is induced in C57BL/6 mice by intraperitoneal injection of 150 μL of pooled sera from adult K/BxN mice.
  • Formulation: 35% TPGS, 60% PEG 400, and 5% propylene glycol
  • Dosages: 1 or 5 mg/kg
  • Administration: Administered orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (159.07 mM)
Water Insoluble
Ethanol 0 mg/mL (0.0 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 628.63
Formula

C22H23FN6O5.C6H6O3S

CAS No. 841290-81-1
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    What’s the difference between S1533 and S2194?

  • Answer:

    S1533 and S2194 are two different forms of R406. S1533 is the free base form, containing only R406 molecule without a acid added to it. S2194 has an additional C6H6O3S acid on it which makes the molecule a salt form. The free base and salt forms have same biology activities. Free base has a lower molecular weight and salt form has a better solubility in DMSO.

Syk Signaling Pathway Map

Syk Inhibitors with Unique Features

Related Syk Products

Tags: buy R406 | R406 supplier | purchase R406 | R406 cost | R406 manufacturer | order R406 | R406 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID