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 MnzaSpVv[3Srb36gRZN{[Xl? MmrjNUDPxE1? M2T1b|PDqGh? MUHy[YR2[2W|IH3p[5JifGmxbtMg MlzTNlYzPTF5NkG=
U266 MkfQSpVv[3Srb36gRZN{[Xl? NGO3OZMyKM7:TR?= MUGzxsBp MVjy[YR2[2W|IH3p[5JifGmxbtMg MnXlNlYzPTF5NkG=
Jeko-1 MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH1XYY1QCCq M{KxcWlEPTB;NT6wOlgzPiEQvF2= M{jXcFI2QDN3N{W1
Mino NIrVUmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm0PEBp NGjtNmVKSzVyPUWuO|A5PTRizszN M1nrWlI2QDN3N{W1
Jeko-1 NEnhUGRCeG:ydH;zbZMhSXO|YYm= NWPoVmJwPcLizszN MnO5NlQhcA>? NFvQXZBqdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz M1jMTVI2QDN3N{W1
primary MCL M2fOeWFxd3C2b4Ppd{BCe3OjeR?= NV7SV4o5OiEEtV2= NIDyfHkzPCCq M1i1W4lv[3KnYYPld{B{cWewaX\pZ4FvfGy7IHHwc5B1d3Orc9Mg MojjNlU{QDh|N{O=
PBMCs M325bGNmdGxiVnnhZoltcXS7IFHzd4F6 M2jvXVAuPTBizszN NUTlS5hNOjRiaB?= MlW0SG1UVw>? NXe0cYhZcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MYWyOVEzPzh4Mh?=
PBMCs MXvGeY5kfGmxbjDBd5NigQ>? MXu1JO69VQ>? NWe5NpJvOSCq MmjPSG1UVw>? NVXYWm5r\GWlcnXhd4V{KHSqZTDj[YxtKG2rZ4LheIlwdg>? NIP6PHkzPTF{N{i2Ni=>
CFSE-CD4+ T  NI\IfI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKwMlA3OjVvMTFOwG0> MWW0JIQ> MkexZoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? NEHCb2kzPDZ5OUm4Ni=>
CFSE-CD11b+ NXPYWGN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUK3fHczOC5yNkK1MVEh|ryP MnTVPEBl NH[xSnVjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= M3zkd|I1Pjd7OUiy
HMECs MWrGeY5kfGmxbjDBd5NigQ>? MUWwMVExKM7:TR?= MnPaNlAhdWmw MkTHbY5pcWKrdIOgWmVITi2|dHnteYxifGWmIILlcIVie2Vib3[gUm8> NH:2bWMzPDN{OUW0OC=>
AB5 MmLFRZBweHSxc3nzJGF{e2G7 MX:wMVIvPSEQvF2= NVPodJpTPDhiaB?= NGnoPYZFVVOR MV\pcoR2[2W|IHHwc5B1d3Orcx?= NXjtO49yOjN|OUi5NVE>
JB7 Ml7vRZBweHSxc3nzJGF{e2G7 NFz5OlQxNTJwNTFOwG0> MlnYOFghcA>? MlPUSG1UVw>? M1rNS4lv\HWlZYOgZZBweHSxc3nz NILx[nIzOzN7OEmxNS=>
AB5 M3:0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPqOI5XOC1{LkWg{txO MWq0PEBp NUTKPFlLTE2VTx?= NI\uNmxqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NVSzemhbOjN|OUi5NVE>
JB7 MmC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD1[|dUOC1{LkWg{txO NWnWOItzPDhiaB?= NIrDeZpFVVOR M{noZ4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NXXEd2ZGOjN|OUi5NVE>
RL NFXNXHJHfW6ldHnvckBCe3OjeR?= M{n2TFIvPS93IN88US=> MYeyOE81QCCq M2fQVmROW09? NVjxUFZ5cW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= NX;SSFlEOjF7Mk[5OlU>
RL MY\GeY5kfGmxbjDBd5NigQ>? NFO2R4UyNzJwNTFOwG0> MX6yOEBp NUnkOWlSTE2VTx?= NVzU[3hGemWmdXPld{B1cGViYXP0bZZifGmxbjDv[kBCc3RiYX7kJJA4OFN4Sx?= MUSyNVkzPjl4NR?=
platelet  NWXhU29TTnWwY4Tpc44hSXO|YYm= M2HMT|HDqM7:bR?= NF;J[no2KG2rbh?= NGjKdHdqdmirYnn0d{BH[87|UlnJRU1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdg>? MlTBNlE5PDh4OUS=
platelet  M4\GS2Z2dmO2aX;uJGF{e2G7 NH7zPG4xNjB3L{GvNk42KM7:TR?= MYW1JI1qdg>? MYDpcohq[mm2czD0bIUhe2mpbnHsbY5oKG2nY3jhcol{dXNiZH;3cpN1emWjbTDv[kBH[87|UlnJRS=> MWeyNVg1QDZ7NB?=
DoHH2 MnLDRZBweHSxc3nzJGF{e2G7 M3vpOlAwOy9zMDFOwG0> MY[0PEBp MW\pcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MWSyNFg4PTRyOB?=
Jeko-1  NIfXPIJCeG:ydH;zbZMhSXO|YYm= NXPlcmdWOC9|L{GwJO69VQ>? NIi0dJQ1QCCq NWDUVoN4cW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= M4K3VVIxQDd3NEC4
Raji  NVm0Z4hjSXCxcITvd4l{KEG|c3H5 MV[wM|MwOTBizszN M1zO[|Q5KGh? M1fRXYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NHe4dJQzODh5NUSwPC=>
DHL4 MVrBdI9xfG:|aYOgRZN{[Xl? MXOwM|EwPCEQvF2= M2DyW|k3KGh? NXTG[2s1cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MYOxPFAxPjZ7Nh?=
LY7 NV\aN2drSXCxcITvd4l{KEG|c3H5 M3zXN|AwOS92IN88US=> MlnUPVYhcA>? NXHHVpdlcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NG\we4YyQDByNk[5Oi=>
LY3 NWTuT20xSXCxcITvd4l{KEG|c3H5 M{nUXFAwOS92IN88US=> MUO5OkBp MlO2bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHHYdpMyQDByNk[5Oi=>
DHL6 MlP3RZBweHSxc3nzJGF{e2G7 M2TpWlAwOS92IN88US=> NX;VcoUxQTZiaB?= Ml\0bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NXL4S5BPOThyME[2PVY>
LY10 Mn[2RZBweHSxc3nzJGF{e2G7 M4DVfFAwOS92IN88US=> NXj2fXFCQTZiaB?= MoHwbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M4TINVE5ODB4Nkm2
DHL10 MkXlRZBweHSxc3nzJGF{e2G7 NXzlcI04OC9zL{Sg{txO NVPIXmNoQTZiaB?= NUW1NFNKcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M4LZWlE5ODB4Nkm2
Wsu-NHL MnrRRZBweHSxc3nzJGF{e2G7 M4\nbVAwOS92IN88US=> NEDofGY6PiCq MoPTbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHfzdFEyQDByNk[5Oi=>
LY18 NI\PVo1CeG:ydH;zbZMhSXO|YYm= MVqwM|EwPCEQvF2= NGTSdG06PiCq NHjEbFlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4TBNVE5ODB4Nkm2
LY1 NIK3XYpCeG:ydH;zbZMhSXO|YYm= NFTOOJQxNzFxNDFOwG0> NHrMenM6PiCq MWDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MkjSNVgxODZ4OU[=
DHL8 Ml73RZBweHSxc3nzJGF{e2G7 M{jz[|AwOS92IN88US=> M{jScFk3KGh? MYDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NU\5cWR5OThyME[2PVY>
DHL4 M4rt[WFxd3C2b4Ppd{BCe3OjeR?= M2O2UlQh|ryP NGfsUpI6PiCq MXLpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MoTVNVgxODZ4OU[=
DHL6 MWfBdI9xfG:|aYOgRZN{[Xl? MniyOEDPxE1? MXK5OkBp M3m0N4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MVmxPFAxPjZ7Nh?=
LY3 MmHTRZBweHSxc3nzJGF{e2G7 M1y5PFQh|ryP NIjLRnI6PiCq M2jC[olv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MUOxPFAxPjZ7Nh?=
LY7 NWXkPYFQSXCxcITvd4l{KEG|c3H5 M4TvbVQh|ryP MYe5OkBp NVS2OHlKcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MkHoNVgxODZ4OU[=
DHL4 MXXGeY5kfGmxbjDBd5NigQ>? M3rvZlQh|ryP NGjydZoyPiCq MVPpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MWOxPFAxPjZ7Nh?=
LY7 M3G2WmZ2dmO2aX;uJGF{e2G7 NITqNJI1KM7:TR?= M2TtfVE3KGh? NFPsWoJqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NWjtZpNuOThyME[2PVY>
LY3 MkPPSpVv[3Srb36gRZN{[Xl? MWC0JO69VQ>? NF7TNVEyPiCq NX;ITY16cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MnS4NVgxODZ4OU[=
DHL6 MmLsSpVv[3Srb36gRZN{[Xl? MYm0JO69VQ>? Ml21NVYhcA>? M4S2cIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M1XEXFE5ODB4Nkm2
LY10 M1jsXmZ2dmO2aX;uJGF{e2G7 MXW0JO69VQ>? NVPuN2JFOTZiaB?= MUTpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NFfNOpYyQDByNk[5Oi=>
Wsu-NHL NX;WdINqTnWwY4Tpc44hSXO|YYm= NHjVdo81KM7:TR?= NV\TOY1[OTZiaB?= MX\pcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NIHqNIQyQDByNk[5Oi=>
LY18 NInJdo5HfW6ldHnvckBCe3OjeR?= MWO0JO69VQ>? NXXuOWpHOTZiaB?= NITweVlqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> M4fUVVE5ODB4Nkm2

... 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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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID