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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4 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.

    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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NYr3c2JTTnWwY4Tpc44hSXO|YYm= MlTMNUDPxE1? NILPT48{yqCq M1mwXpJm\HWlZYOgcYloemG2aX;uxsA> NF6wb3gzPjJ3MUe2NS=>
U266 NFHhb4xHfW6ldHnvckBCe3OjeR?= NHi5[3YyKM7:TR?= NH;RUZY{yqCq NHvS[XFz\WS3Y3XzJI1q\3KjdHnvcuKh NF;hSlEzPjJ3MUe2NS=>
Jeko-1 M3KzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLwUW41QCCq NYDYPYRlUUN3ME21MlA3QDJ4IN88US=> M2qwR|I2QDN3N{W1
Mino MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jyWFQ5KGh? NH\sZnpKSzVyPUWuO|A5PTRizszN NYe3cWpnOjV6M{W3OVU>
Jeko-1 M1vKXmFxd3C2b4Ppd{BCe3OjeR?= M2LoRVXDqM7:TR?= MmHvNlQhcA>? MYLpcoR2[2W|IEK1MlHDqMLzwrCzMlLDqCViYYDvdJRwe2m| MXmyOVg{PTd3NR?=
primary MCL M4LBOWFxd3C2b4Ppd{BCe3OjeR?= NHrsfWUzKML3TR?= Mlz4NlQhcA>? MkLHbY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= M4PONlI2Ozh6M{ez
PBMCs M2CyOGNmdGxiVnnhZoltcXS7IFHzd4F6 NGHyUGkxNTVyIN88US=> MW[yOEBp M3fxe2ROW09? MY\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MX:yOVEzPzh4Mh?=
PBMCs M3;hTGZ2dmO2aX;uJGF{e2G7 MlfIOUDPxE1? M1:3dVEhcA>? NVL0botQTE2VTx?= MYPk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u MlfmNlUyOjd6NkK=
CFSE-CD4+ T  MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWwMlA3OjVvMTFOwG0> MXG0JIQ> NFrI[WNjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= MnzvNlQ3Pzl7OEK=
CFSE-CD11b+ Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\VNE4xPjJ3LUGg{txO MkLVPEBl M3HqPYJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| MlTvNlQ3Pzl7OEK=
HMECs M2f3eGZ2dmO2aX;uJGF{e2G7 M1\VPVAuOTBizszN NFLqR3EzOCCvaX6= NVPvPZlpcW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? Ml7RNlQ{Ojl3NES=
AB5 M3[0eWFxd3C2b4Ppd{BCe3OjeR?= MX2wMVIvPSEQvF2= MWC0PEBp M4e3XGROW09? M3K0fYlv\HWlZYOgZZBweHSxc3nz NWn6T3VsOjN|OUi5NVE>
JB7 NWniUW05SXCxcITvd4l{KEG|c3H5 Mln0NE0zNjVizszN NYnaV3dTPDhiaB?= M17uNWROW09? NXrzU214cW6mdXPld{BieG:ydH;zbZM> NGr2bnYzOzN7OEmxNS=>
AB5 M17zSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[wMVIvPSEQvF2= M{\JSlQ5KGh? NHfYeo5FVVOR MlrGbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M3;EfFI{Ozl6OUGx
JB7 NWf0SWtET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LuW|AuOi53IN88US=> M2Xye|Q5KGh? MkmySG1UVw>? MWnpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NXTWXFlQOjN|OUi5NVE>
RL NWq3eXg5TnWwY4Tpc44hSXO|YYm= Ml7jNk42NzVizszN MlXNNlQwPDhiaB?= NHKzSm5FVVOR NWfTSJpIcW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= MUKyNVkzPjl4NR?=
RL NWXGe2NTTnWwY4Tpc44hSXO|YYm= M4HmZlEwOi53IN88US=> NFvINGUzPCCq NIK2NGtFVVOR M2G0UpJm\HWlZYOgeIhmKGGldHn2ZZRqd25ib3[gRYt1KGGwZDDwO|BUPkt? MWmyNVkzPjl4NR?=
platelet  NF60cphHfW6ldHnvckBCe3OjeR?= MnHINeKh|ryv M3XN[|UhdWmw MWrpcohq[mm2czDGZ:6{WkmLQT3t[YRq[XSnZDDwcIF1\WyndDDh[4dz\WejdHnvci=> NEXTcVMzOTh2OE[5OC=>
platelet  MVLGeY5kfGmxbjDBd5NigQ>? MnPrNE4xPS9zL{KuOUDPxE1? M2rJ[lUhdWmw M3nifYlvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC MXqyNVg1QDZ7NB?=
DoHH2 M2PLT2Fxd3C2b4Ppd{BCe3OjeR?= NVvmVlZEOC9|L{GwJO69VQ>? MWC0PEBp MUXpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? M3XhblIxQDd3NEC4
Jeko-1  NFTiT2pCeG:ydH;zbZMhSXO|YYm= NVTFTZVbOC9|L{GwJO69VQ>? NInaN5g1QCCq M4SzVYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 MnrNNlA5PzV2MEi=
Raji  NHjzdnBCeG:ydH;zbZMhSXO|YYm= M2XBcVAwOy9zMDFOwG0> MVe0PEBp NEe5OYdqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= M3GzdVIxQDd3NEC4
DHL4 M4fQWmFxd3C2b4Ppd{BCe3OjeR?= M1u0S|AwOS92IN88US=> M4P5WVk3KGh? NEDsRpRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVS0NoJGOThyME[2PVY>
LY7 M{fuVGFxd3C2b4Ppd{BCe3OjeR?= NYjQfWlSOC9zL{Sg{txO NVvScmxjQTZiaB?= Mor1bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MnnHNVgxODZ4OU[=
LY3 MoTnRZBweHSxc3nzJGF{e2G7 NGf6N4sxNzFxNDFOwG0> NX7pZXdYQTZiaB?= M1fjd4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Mn7tNVgxODZ4OU[=
DHL6 M1XobmFxd3C2b4Ppd{BCe3OjeR?= Mnz1NE8yNzRizszN NYLPZ|MzQTZiaB?= M{TpN4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NF\pSIsyQDByNk[5Oi=>
LY10 Mnm4RZBweHSxc3nzJGF{e2G7 M1PV[FAwOS92IN88US=> MofmPVYhcA>? MmLmbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MkK0NVgxODZ4OU[=
DHL10 M{Tyc2Fxd3C2b4Ppd{BCe3OjeR?= NH36XHQxNzFxNDFOwG0> NYnySYQ{QTZiaB?= MorQbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= Ml30NVgxODZ4OU[=
Wsu-NHL MmS3RZBweHSxc3nzJGF{e2G7 M2DrO|AwOS92IN88US=> NYDmc5MzQTZiaB?= MlvwbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M4P2flE5ODB4Nkm2
LY18 NFSwemZCeG:ydH;zbZMhSXO|YYm= Ml[0NE8yNzRizszN MYC5OkBp NV;sNlZGcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NHvTZ2EyQDByNk[5Oi=>
LY1 MoHiRZBweHSxc3nzJGF{e2G7 NFWwfJcxNzFxNDFOwG0> M4fYd|k3KGh? NGTiUXlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4T5bFE5ODB4Nkm2
DHL8 M4ezNWFxd3C2b4Ppd{BCe3OjeR?= NFjtXpIxNzFxNDFOwG0> NITCNIY6PiCq NIXs[oxqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NGPSR4cyQDByNk[5Oi=>
DHL4 NYHmUnJqSXCxcITvd4l{KEG|c3H5 Mlf2OEDPxE1? Mn76PVYhcA>? M3;QNIlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NI[0Z|MyQDByNk[5Oi=>
DHL6 MoDSRZBweHSxc3nzJGF{e2G7 NXXidFdHPCEQvF2= MYO5OkBp MUHpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MVWxPFAxPjZ7Nh?=
LY3 MWXBdI9xfG:|aYOgRZN{[Xl? NWXLbHM3PCEQvF2= NXKyWlJwQTZiaB?= NFP6PY5qdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NXfNbFd1OThyME[2PVY>
LY7 NVPXdJFuSXCxcITvd4l{KEG|c3H5 NVr2TIhjPCEQvF2= MWS5OkBp M{\kdYlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MWKxPFAxPjZ7Nh?=
DHL4 M1y5bWZ2dmO2aX;uJGF{e2G7 MoPZOEDPxE1? MXKxOkBp MnnSbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NYTVSpVFOThyME[2PVY>
LY7 NH:1UIFHfW6ldHnvckBCe3OjeR?= NGPlPXM1KM7:TR?= NFrxNXUyPiCq M3XZcIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NUTpXVg4OThyME[2PVY>
LY3 MlLvSpVv[3Srb36gRZN{[Xl? MlztOEDPxE1? NWfZ[Xd1OTZiaB?= M{HXRYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NHryV3AyQDByNk[5Oi=>
DHL6 NInucHhHfW6ldHnvckBCe3OjeR?= NH7HelQ1KM7:TR?= NY\H[YprOTZiaB?= MVzpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NV\iWIlvOThyME[2PVY>
LY10 M2fVfWZ2dmO2aX;uJGF{e2G7 NGPvcXQ1KM7:TR?= MWSxOkBp NXTPUZVjcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NGjNVmYyQDByNk[5Oi=>
Wsu-NHL M1vYdGZ2dmO2aX;uJGF{e2G7 MV:0JO69VQ>? MUmxOkBp MYDpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NGP3cmYyQDByNk[5Oi=>
LY18 NF\Ob2xHfW6ldHnvckBCe3OjeR?= M2G5fFQh|ryP MXuxOkBp NUjGXmlqcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MlXKNVgxODZ4OU[=

... 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 126 mg/mL (200.43 mM)
Ethanol 8 mg/mL (12.72 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% Propylene glycol 30mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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