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 M3uxSmZ2dmO2aX;uJGF{e2G7 NHX3NGYyKM7:TR?= MXmzxsBp M3fXU5Jm\HWlZYOgcYloemG2aX;uxsA> MmDCNlYzPTF5NkG=
U266 M3Ti[mZ2dmO2aX;uJGF{e2G7 M2fTRVEh|ryP MW[zxsBp NETT[3Nz\WS3Y3XzJI1q\3KjdHnvcuKh MVeyOlI2OTd4MR?=
Jeko-1 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\GcW5[PDhiaB?= MU\JR|UxRTVwME[4NlYh|ryP NUL0ZpJZOjV6M{W3OVU>
Mino M1:2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4SxU|Q5KGh? MYnJR|UxRTVwN{C4OVQh|ryP MmTzNlU5OzV5NUW=
Jeko-1 MY\BdI9xfG:|aYOgRZN{[Xl? MX:1xsDPxE1? NVXLdFZQOjRiaB?= NEf2NodqdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz M4HxVFI2QDN3N{W1
primary MCL MX3BdI9xfG:|aYOgRZN{[Xl? M2jkZlIhyrWP MlS4NlQhcA>? NHXpWY1qdmO{ZXHz[ZMhe2mpbnnmbYNidnSueTDhdI9xfG:|aYRCpC=> MmTjNlU{QDh|N{O=
PBMCs NHHnNVRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1fpOVAuPTBizszN NGm3eVAzPCCq NGfnN2hFVVOR MVnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4HrfVI2OTJ5OE[y
PBMCs NFzZV|ZHfW6ldHnvckBCe3OjeR?= NFrPVpo2KM7:TR?= MU[xJIg> NHz3[XBFVVOR Mkm5[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> NIDYWXEzPTF{N{i2Ni=>
CFSE-CD4+ T  Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGOyT2IxNjB4MkWtNUDPxE1? MlLYOEBl MX3icI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? MYmyOFY4QTl6Mh?=
CFSE-CD11b+ M1XvSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;GVVcxNjB4MkWtNUDPxE1? NHK1em05KGR? M1:0WIJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| M1;OZlI1Pjd7OUiy
HMECs NIGxcZNHfW6ldHnvckBCe3OjeR?= NILm[|AxNTFyIN88US=> M3\ab|IxKG2rbh?= NXTSbWFPcW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? MWqyOFMzQTV2NB?=
AB5 MX3BdI9xfG:|aYOgRZN{[Xl? MoLBNE0zNjVizszN NHnXTmM1QCCq NVr6WJYxTE2VTx?= MVPpcoR2[2W|IHHwc5B1d3Orcx?= NVHhd5JKOjN|OUi5NVE>
JB7 MYfBdI9xfG:|aYOgRZN{[Xl? MYSwMVIvPSEQvF2= MojXOFghcA>? MX7EUXNQ NH\SeYdqdmS3Y3XzJIFxd3C2b4Ppdy=> M1jkZlI{Ozl6OUGx
AB5 NGXJPIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWwMVIvPSEQvF2= NYrsPJRQPDhiaB?= NIPET|lFVVOR NHu1PWxqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NF;pbFQzOzN7OEmxNS=>
JB7 NI\IVnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LZSlAuOi53IN88US=> NX7PdJd[PDhiaB?= NUe3OJozTE2VTx?= M{nQ[4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M2[1UlI{Ozl6OUGx
RL MUTGeY5kfGmxbjDBd5NigQ>? NVT3eXAyOi53L{Wg{txO NFezXG4zPC92ODDo NFyyU2tFVVOR NXnQVZpncW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= NV6zTFRYOjF7Mk[5OlU>
RL MWfGeY5kfGmxbjDBd5NigQ>? MlnVNU8zNjVizszN M2Gw[FI1KGh? NEG4TZVFVVOR MlzodoVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? M{\IelIyQTJ4OU[1
platelet  M2jzXmZ2dmO2aX;uJGF{e2G7 NWDHRXl5OcLizszt M{\k[VUhdWmw NX3z[m5ZcW6qaXLpeJMhTmQQs2LJTWEudWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25? MYGyNVg1QDZ7NB?=
platelet  MV\GeY5kfGmxbjDBd5NigQ>? NU\CTndPOC5yNT:xM|IvPSEQvF2= NHr5[2k2KG2rbh?= M33rUYlvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC NWXBUZFLOjF6NEi2PVQ>
DoHH2 MUnBdI9xfG:|aYOgRZN{[Xl? NXnWOGtqOC9|L{GwJO69VQ>? NIPheIs1QCCq NXvMd5JjcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MWOyNFg4PTRyOB?=
Jeko-1  NIrMOpdCeG:ydH;zbZMhSXO|YYm= MUKwM|MwOTBizszN NHrsUok1QCCq MmPCbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? NGHITlgzODh5NUSwPC=>
Raji  NWXPO21DSXCxcITvd4l{KEG|c3H5 NF3kRXQxNzNxMUCg{txO NVfHXY15PDhiaB?= MUPpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MlTuNlA5PzV2MEi=
DHL4 M13FR2Fxd3C2b4Ppd{BCe3OjeR?= NYXxWFBrOC9zL{Sg{txO Mm\MPVYhcA>? NVfYZ|d7cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NX7RXlIxOThyME[2PVY>
LY7 M{LUTGFxd3C2b4Ppd{BCe3OjeR?= NFiz[XoxNzFxNDFOwG0> NGrlXIg6PiCq NI\rN|FqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NH7ofVAyQDByNk[5Oi=>
LY3 MnzIRZBweHSxc3nzJGF{e2G7 NHHtR28xNzFxNDFOwG0> MnTSPVYhcA>? NVLtU2xIcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYT4dmhLOThyME[2PVY>
DHL6 MXfBdI9xfG:|aYOgRZN{[Xl? NGnqWpkxNzFxNDFOwG0> NIfpcow6PiCq Mmq2bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MX6xPFAxPjZ7Nh?=
LY10 NFnYXFZCeG:ydH;zbZMhSXO|YYm= MUSwM|EwPCEQvF2= NX:zbI9NQTZiaB?= MVXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MlLBNVgxODZ4OU[=
DHL10 M3r5NmFxd3C2b4Ppd{BCe3OjeR?= Mm\xNE8yNzRizszN NFjUeZY6PiCq M{DW[Ylv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NXvQcYxuOThyME[2PVY>
Wsu-NHL MYjBdI9xfG:|aYOgRZN{[Xl? M4OxdVAwOS92IN88US=> MUi5OkBp MYXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NUjMb4tHOThyME[2PVY>
LY18 Mo\WRZBweHSxc3nzJGF{e2G7 NU\Hd5Q{OC9zL{Sg{txO NXfrUGd{QTZiaB?= NYnQT3BQcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NIT5UnEyQDByNk[5Oi=>
LY1 MoTCRZBweHSxc3nzJGF{e2G7 NXHOR2NtOC9zL{Sg{txO MVO5OkBp NGnVTHNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MonhNVgxODZ4OU[=
DHL8 NWD6dmVWSXCxcITvd4l{KEG|c3H5 MVKwM|EwPCEQvF2= M4PxT|k3KGh? MnzPbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NGn4bWYyQDByNk[5Oi=>
DHL4 NYP3OGVsSXCxcITvd4l{KEG|c3H5 M17RWVQh|ryP NWrBb|ZYQTZiaB?= M3f3VIlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> Mo\KNVgxODZ4OU[=
DHL6 MYPBdI9xfG:|aYOgRZN{[Xl? M3;ZOFQh|ryP NFfM[nk6PiCq M1i3[olv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NFe2cmUyQDByNk[5Oi=>
LY3 Mn\hRZBweHSxc3nzJGF{e2G7 NX3q[XVZPCEQvF2= NIjVN2g6PiCq M4nocYlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MkTJNVgxODZ4OU[=
LY7 NHL3OlZCeG:ydH;zbZMhSXO|YYm= NWfUVXBuPCEQvF2= M4XkUlk3KGh? NEO2bJpqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MnzFNVgxODZ4OU[=
DHL4 NILqW4hHfW6ldHnvckBCe3OjeR?= NVjJSII5PCEQvF2= NY\abYZlOTZiaB?= NWrPeGFPcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MkDsNVgxODZ4OU[=
LY7 MV;GeY5kfGmxbjDBd5NigQ>? NEX6fZM1KM7:TR?= M{XtZVE3KGh? M3HueIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u Mn32NVgxODZ4OU[=
LY3 NHLW[mxHfW6ldHnvckBCe3OjeR?= NHHnPI41KM7:TR?= NWL0[45xOTZiaB?= NGnJO2JqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MV:xPFAxPjZ7Nh?=
DHL6 M4[x[WZ2dmO2aX;uJGF{e2G7 MkPvOEDPxE1? NHzDWmkyPiCq M3XwZolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NXf5VlVlOThyME[2PVY>
LY10 NYLRVld1TnWwY4Tpc44hSXO|YYm= MnryOEDPxE1? NWnmWlBmOTZiaB?= MVHpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MUixPFAxPjZ7Nh?=
Wsu-NHL NXH0SYNxTnWwY4Tpc44hSXO|YYm= MnuyOEDPxE1? MUCxOkBp Mn7vbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NV\YeIlNOThyME[2PVY>
LY18 NYKxXnNuTnWwY4Tpc44hSXO|YYm= MYe0JO69VQ>? M33iVVE3KGh? NEjUOJhqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MYWxPFAxPjZ7Nh?=

... 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