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
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5 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.

  • 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

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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 MX7GeY5kfGmxbjDBd5NigQ>? M2PWWFEh|ryP MmjMN:KhcA>? NETRTo5z\WS3Y3XzJI1q\3KjdHnvcuKh MmHXNlYzPTF5NkG=
U266 NH3RO3ZHfW6ldHnvckBCe3OjeR?= MXqxJO69VQ>? NILPfHU{yqCq NXvxOWJpemWmdXPld{BucWe{YYTpc47DqA>? M2PXb|I3OjVzN{[x
Jeko-1 NH76RpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYC0PEBp NFzkdZlKSzVyPUWuNFY5OjZizszN M3faT|I2QDN3N{W1
Mino MnjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LhWVQ5KGh? NGHGU5JKSzVyPUWuO|A5PTRizszN MU[yOVg{PTd3NR?=
Jeko-1 NX;KPWtVSXCxcITvd4l{KEG|c3H5 NXTwVW55PcLizszN NGTZb|QzPCCq M1XUWolv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= Mk\0NlU5OzV5NUW=
primary MCL M2nWNGFxd3C2b4Ppd{BCe3OjeR?= M2DQW|IhyrWP MYWyOEBp MW\pcoNz\WG|ZYOgd4lodmmoaXPhcpRtgSCjcH;weI9{cXQEoB?= NIH5ZYgzPTN6OEO3Ny=>
PBMCs M{LicmNmdGxiVnnhZoltcXS7IFHzd4F6 NW\wTXk{OC13MDFOwG0> MYWyOEBp NIHWNXBFVVOR NVfEeY1LcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXLHeY8{OjVzMke4OlI>
PBMCs M3;OV2Z2dmO2aX;uJGF{e2G7 MUO1JO69VQ>? MnPtNUBp M{TNe2ROW09? MoX6[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> NXHoelNDOjVzMke4OlI>
CFSE-CD4+ T  M{ntRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2wMlA3OjVvMTFOwG0> NIrVTW81KGR? Mmq4Zoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? NWKyWWR6OjR4N{m5PFI>
CFSE-CD11b+ MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjQVJMxNjB4MkWtNUDPxE1? MWS4JIQ> MlTrZoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? MoGyNlQ3Pzl7OEK=
HMECs Mnu2SpVv[3Srb36gRZN{[Xl? MUGwMVExKM7:TR?= MkPvNlAhdWmw Ml7DbY5pcWKrdIOgWmVITi2|dHnteYxifGWmIILlcIVie2Vib3[gUm8> NX\ne45zOjR|Mkm1OFQ>
AB5 NXfCfGhxSXCxcITvd4l{KEG|c3H5 MknFNE0zNjVizszN M13J[FQ5KGh? MlLXSG1UVw>? MlzSbY5lfWOnczDhdI9xfG:|aYO= NITLOoEzOzN7OEmxNS=>
JB7 NGjmOppCeG:ydH;zbZMhSXO|YYm= M2DBelAuOi53IN88US=> NXLSd|BbPDhiaB?= MlHtSG1UVw>? MWrpcoR2[2W|IHHwc5B1d3Orcx?= M3LzSlI{Ozl6OUGx
AB5 NVT0bFU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWz[nFSOC1{LkWg{txO MmrvOFghcA>? NWrDNmhQTE2VTx?= M4LRc4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M2\ITVI{Ozl6OUGx
JB7 M2HIOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i4flAuOi53IN88US=> NVz6TFEyPDhiaB?= M{W2RmROW09? MnT6bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M4nh[|I{Ozl6OUGx
RL MX;GeY5kfGmxbjDBd5NigQ>? NVXvfnZzOi53L{Wg{txO NUDoTGhiOjRxNEigbC=> MlfsSG1UVw>? MoK2bY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? MlTpNlE6OjZ7NkW=
RL Mn\KSpVv[3Srb36gRZN{[Xl? NXHXSoc2OS9{LkWg{txO MnLNNlQhcA>? NXHQ[HdWTE2VTx?= M{LRU5Jm\HWlZYOgeIhmKGGldHn2ZZRqd25ib3[gRYt1KGGwZDDwO|BUPkt? MWSyNVkzPjl4NR?=
platelet  NIf1WppHfW6ldHnvckBCe3OjeR?= Ml[3NeKh|ryv M4fPSFUhdWmw NXHQbZE1cW6qaXLpeJMhTmQQs2LJTWEudWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25? NICyVlgzOTh2OE[5OC=>
platelet  NFjOWHFHfW6ldHnvckBCe3OjeR?= NFW0V2MxNjB3L{GvNk42KM7:TR?= M{LFcVUhdWmw NWL4[XhicW6qaXLpeJMhfGinIIPp[45idGmwZzDt[YNp[W6rc33zJIRwf26|dILlZY0hd2ZiRnROt3JKUUF? MmLHNlE5PDh4OUS=
DoHH2 NEPiXnhCeG:ydH;zbZMhSXO|YYm= NID4O5gxNzNxMUCg{txO MnrlOFghcA>? MWnpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MY[yNFg4PTRyOB?=
Jeko-1  NHX6V2hCeG:ydH;zbZMhSXO|YYm= MmH1NE8{NzFyIN88US=> M2fST|Q5KGh? MoLzbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? MnTlNlA5PzV2MEi=
Raji  NHfwXpRCeG:ydH;zbZMhSXO|YYm= NUXzb4RVOC9|L{GwJO69VQ>? NWTmXWtQPDhiaB?= NV\uUlFUcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NGHiXHQzODh5NUSwPC=>
DHL4 NEPMOYtCeG:ydH;zbZMhSXO|YYm= NGnkXFkxNzFxNDFOwG0> M{jYSFk3KGh? MUXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MmHRNVgxODZ4OU[=
LY7 NGrpSm1CeG:ydH;zbZMhSXO|YYm= MXOwM|EwPCEQvF2= MU[5OkBp NVfjcI96cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NH34OlgyQDByNk[5Oi=>
LY3 MojJRZBweHSxc3nzJGF{e2G7 MUCwM|EwPCEQvF2= NX3RbIQ{QTZiaB?= NXKzXIZGcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MUOxPFAxPjZ7Nh?=
DHL6 NE\rTJpCeG:ydH;zbZMhSXO|YYm= NULBVFAzOC9zL{Sg{txO MVu5OkBp M4f3W4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NIjmfG0yQDByNk[5Oi=>
LY10 MUPBdI9xfG:|aYOgRZN{[Xl? NHnBVpoxNzFxNDFOwG0> M{TiPFk3KGh? Mm\MbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M2\EUFE5ODB4Nkm2
DHL10 NGe1VmpCeG:ydH;zbZMhSXO|YYm= NIH0TJoxNzFxNDFOwG0> M{\aN|k3KGh? NF[5TnBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFnqfG4yQDByNk[5Oi=>
Wsu-NHL NUfxPHN{SXCxcITvd4l{KEG|c3H5 NWHTPJNFOC9zL{Sg{txO NHL3W5Y6PiCq MXXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MUCxPFAxPjZ7Nh?=
LY18 MX\BdI9xfG:|aYOgRZN{[Xl? NGDOZmYxNzFxNDFOwG0> MmHsPVYhcA>? M3TEWYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NFrG[oQyQDByNk[5Oi=>
LY1 MWLBdI9xfG:|aYOgRZN{[Xl? NYXieZVIOC9zL{Sg{txO MlnMPVYhcA>? Mlm1bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M371R|E5ODB4Nkm2
DHL8 NG[wbXlCeG:ydH;zbZMhSXO|YYm= MlvZNE8yNzRizszN MmHpPVYhcA>? NUnkV2VFcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NXezb|FPOThyME[2PVY>
DHL4 MnnFRZBweHSxc3nzJGF{e2G7 NUfrUGpiPCEQvF2= NH3KWIs6PiCq NEn2ZnBqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 M2nLU|E5ODB4Nkm2
DHL6 NV3nTnlMSXCxcITvd4l{KEG|c3H5 MlqyOEDPxE1? NW\r[opJQTZiaB?= NYno[3pzcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MlLyNVgxODZ4OU[=
LY3 MknTRZBweHSxc3nzJGF{e2G7 M1fWdVQh|ryP Mk\sPVYhcA>? MlPTbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MXixPFAxPjZ7Nh?=
LY7 MYLBdI9xfG:|aYOgRZN{[Xl? M4OxelQh|ryP NWPxd413QTZiaB?= NVzlPIJYcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MlLrNVgxODZ4OU[=
DHL4 M2nEcmZ2dmO2aX;uJGF{e2G7 MnzCOEDPxE1? MnTCNVYhcA>? MmPabY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= M3jQSlE5ODB4Nkm2
LY7 MkLuSpVv[3Srb36gRZN{[Xl? NHj2Tm81KM7:TR?= NW[3fJBEOTZiaB?= NYKycnNzcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> Mle2NVgxODZ4OU[=
LY3 MWLGeY5kfGmxbjDBd5NigQ>? MlK1OEDPxE1? NFjNPWEyPiCq Ml[4bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MnrxNVgxODZ4OU[=
DHL6 NVzrSJp{TnWwY4Tpc44hSXO|YYm= M2fuWlQh|ryP NUe1W3FvOTZiaB?= MlmwbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NETrfXYyQDByNk[5Oi=>
LY10 NY\SWGl1TnWwY4Tpc44hSXO|YYm= NYHqVo5jPCEQvF2= NVXweFE1OTZiaB?= M17HXYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MW[xPFAxPjZ7Nh?=
Wsu-NHL MV;GeY5kfGmxbjDBd5NigQ>? Mmm3OEDPxE1? M3LjUVE3KGh? MUDpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NFm1WGgyQDByNk[5Oi=>
LY18 NXvyeWdpTnWwY4Tpc44hSXO|YYm= MoewOEDPxE1? MX:xOkBp NF7uNWpqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NGj5ZWoyQDByNk[5Oi=>

... 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)
Ethanol 8 mg/mL (12.72 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% Propylene glycol
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID