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 MomxSpVv[3Srb36gRZN{[Xl? M{fQV|Eh|ryP NX3LWnRTO8LiaB?= NXWyfHRUemWmdXPld{BucWe{YYTpc47DqA>? MUmyOlI2OTd4MR?=
U266 NVvuPHNDTnWwY4Tpc44hSXO|YYm= MkXsNUDPxE1? M4XmUFPDqGh? M2n5N5Jm\HWlZYOgcYloemG2aX;uxsA> NU\1WW54OjZ{NUG3OlE>
Jeko-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\FUlQ5KGh? M1PTcmlEPTB;NT6wOlgzPiEQvF2= NWrNdJp7OjV6M{W3OVU>
Mino NV\0SWl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\TZ|Q5KGh? MlLCTWM2OD13LkewPFU1KM7:TR?= MoHSNlU5OzV5NUW=
Jeko-1 MluxRZBweHSxc3nzJGF{e2G7 MX61xsDPxE1? NXrHU|ZmOjRiaB?= NUjoVm0ycW6mdXPld{AzPS5zwrFCteKhOy5{wrClJIFxd3C2b4Ppdy=> M2G0XFI2QDN3N{W1
primary MCL MYDBdI9xfG:|aYOgRZN{[Xl? NIjXU5YzKML3TR?= M3nCeFI1KGh? M4[yRolv[3KnYYPld{B{cWewaX\pZ4FvfGy7IHHwc5B1d3Orc9Mg NHLUUGgzPTN6OEO3Ny=>
PBMCs M3XxfGNmdGxiVnnhZoltcXS7IFHzd4F6 NETiNpIxNTVyIN88US=> MVqyOEBp NIfp[3ZFVVOR MWHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NIe4fnIzPTF{N{i2Ni=>
PBMCs M1fQPGZ2dmO2aX;uJGF{e2G7 NVLGell3PSEQvF2= NU[wPZNuOSCq M1\vRmROW09? MV3k[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u MVuyOVEzPzh4Mh?=
CFSE-CD4+ T  M4rQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOwMlA3OjVvMTFOwG0> M1PzXFQh\A>? NInsNWpjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= M4HUNlI1Pjd7OUiy
CFSE-CD11b+ NVrRS4dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHKwb3IxNjB4MkWtNUDPxE1? NYLBNIFsQCCm NITsbWljdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= NVjpfmMyOjR4N{m5PFI>
HMECs NGexN4lHfW6ldHnvckBCe3OjeR?= NVrYclJJOC1zMDFOwG0> MnXCNlAhdWmw NGD5SlFqdmirYnn0d{BXTUeILYP0bY12dGG2ZXSgdoVt\WG|ZTDv[kBPVw>? MWiyOFMzQTV2NB?=
AB5 MU\BdI9xfG:|aYOgRZN{[Xl? M134WFAuOi53IN88US=> NXHFRXZwPDhiaB?= NWW4S29WTE2VTx?= MUfpcoR2[2W|IHHwc5B1d3Orcx?= MUCyN|M6QDlzMR?=
JB7 NWi0[WVqSXCxcITvd4l{KEG|c3H5 NWW3SGdxOC1{LkWg{txO NHWyeGU1QCCq NYTlVJI4TE2VTx?= NF\uSnJqdmS3Y3XzJIFxd3C2b4Ppdy=> MkLJNlM{QTh7MUG=
AB5 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHPcogxNTJwNTFOwG0> MWG0PEBp MVzEUXNQ MoTEbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MWWyN|M6QDlzMR?=
JB7 M2nZXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvW[WsxNTJwNTFOwG0> NYS0UWNsPDhiaB?= NUj4OXgyTE2VTx?= MkfvbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MlKzNlM{QTh7MUG=
RL NXTm[FFDTnWwY4Tpc44hSXO|YYm= NI\pd|kzNjVxNTFOwG0> MkLkNlQwPDhiaB?= M2X0e2ROW09? NWXGUpdtcW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= NIrMbVkzOTl{Nkm2OS=>
RL M2nWZ2Z2dmO2aX;uJGF{e2G7 NXL3coZYOS9{LkWg{txO NWnCUIpJOjRiaB?= MnrhSG1UVw>? MmXndoVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? MXiyNVkzPjl4NR?=
platelet  Mk\MSpVv[3Srb36gRZN{[Xl? NWHtSY5DOcLizszt M4P3fVUhdWmw MmP6bY5pcWKrdIOgSoPPu1KLSVGtcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44> NYLXVGt[OjF6NEi2PVQ>
platelet  MXzGeY5kfGmxbjDBd5NigQ>? NHfzXo0xNjB3L{GvNk42KM7:TR?= MYm1JI1qdg>? M2DGPIlvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC NFfrSpAzOTh2OE[5OC=>
DoHH2 MUfBdI9xfG:|aYOgRZN{[Xl? M4HTUFAwOy9zMDFOwG0> MmPMOFghcA>? M3\QVIlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NX\HcpJOOjB6N{W0NFg>
Jeko-1  M{fRZmFxd3C2b4Ppd{BCe3OjeR?= NHPmXVYxNzNxMUCg{txO MWC0PEBp M2rpOYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NEfjXGgzODh5NUSwPC=>
Raji  NHiyeGRCeG:ydH;zbZMhSXO|YYm= MmjvNE8{NzFyIN88US=> M4\PS|Q5KGh? NWry[lk6cW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= M4\iVlIxQDd3NEC4
DHL4 NFXwXmZCeG:ydH;zbZMhSXO|YYm= NWPGN2FOOC9zL{Sg{txO M{eyW|k3KGh? MlX6bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MXuxPFAxPjZ7Nh?=
LY7 MVPBdI9xfG:|aYOgRZN{[Xl? NGTiZXoxNzFxNDFOwG0> NUjsXoRsQTZiaB?= MkHzbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NGDEeYMyQDByNk[5Oi=>
LY3 M33OfGFxd3C2b4Ppd{BCe3OjeR?= M4m5dlAwOS92IN88US=> M{\uTlk3KGh? M376T4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MoX5NVgxODZ4OU[=
DHL6 Mmr3RZBweHSxc3nzJGF{e2G7 Mn3TNE8yNzRizszN NEXMbIs6PiCq M4DWb4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NHnRcnUyQDByNk[5Oi=>
LY10 M{PiXGFxd3C2b4Ppd{BCe3OjeR?= MUGwM|EwPCEQvF2= M3LwZ|k3KGh? MWDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MoW1NVgxODZ4OU[=
DHL10 NFfLTINCeG:ydH;zbZMhSXO|YYm= NYW5Z5hxOC9zL{Sg{txO NFXNW|Y6PiCq M3fpRolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M13rWFE5ODB4Nkm2
Wsu-NHL MUDBdI9xfG:|aYOgRZN{[Xl? NIfadXQxNzFxNDFOwG0> MmXzPVYhcA>? NGfRRYFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M37vdlE5ODB4Nkm2
LY18 NXPSXplzSXCxcITvd4l{KEG|c3H5 NYfhbYVrOC9zL{Sg{txO MnXGPVYhcA>? Mlq4bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M3q2fFE5ODB4Nkm2
LY1 MX\BdI9xfG:|aYOgRZN{[Xl? MoXHNE8yNzRizszN MmjGPVYhcA>? M4HaT4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1S0[lE5ODB4Nkm2
DHL8 NV20UYxpSXCxcITvd4l{KEG|c3H5 NV;lbYhmOC9zL{Sg{txO NEmzWlc6PiCq NGnYeItqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NET2eGcyQDByNk[5Oi=>
DHL4 MkO1RZBweHSxc3nzJGF{e2G7 Ml;jOEDPxE1? NH[1V|A6PiCq NH73WG1qdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 M4LaUlE5ODB4Nkm2
DHL6 MoOwRZBweHSxc3nzJGF{e2G7 MoPWOEDPxE1? NFzGdJU6PiCq NUTKOYFUcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MWmxPFAxPjZ7Nh?=
LY3 NXzqSGlpSXCxcITvd4l{KEG|c3H5 NV7zcI9mPCEQvF2= NX\o[oxLQTZiaB?= MlThbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> NHX0U5oyQDByNk[5Oi=>
LY7 NF;UPWNCeG:ydH;zbZMhSXO|YYm= MljNOEDPxE1? MW[5OkBp MX3pcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MYqxPFAxPjZ7Nh?=
DHL4 NXHPN|hiTnWwY4Tpc44hSXO|YYm= NIPEXnA1KM7:TR?= MV[xOkBp NUXhN3hbcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> M4C4dVE5ODB4Nkm2
LY7 NEXwNYpHfW6ldHnvckBCe3OjeR?= MYG0JO69VQ>? MYixOkBp MYrpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MWixPFAxPjZ7Nh?=
LY3 Mk\DSpVv[3Srb36gRZN{[Xl? MkP3OEDPxE1? NHLkVVUyPiCq NWWwdG4xcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NV7adZFXOThyME[2PVY>
DHL6 NY\pXXhDTnWwY4Tpc44hSXO|YYm= M2LZelQh|ryP MYixOkBp M{ftO4lvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MVWxPFAxPjZ7Nh?=
LY10 MXzGeY5kfGmxbjDBd5NigQ>? M3rMO|Qh|ryP MVGxOkBp NH\BRllqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MVqxPFAxPjZ7Nh?=
Wsu-NHL MmH2SpVv[3Srb36gRZN{[Xl? NIjUOWg1KM7:TR?= NGfQXYwyPiCq MVvpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NH3WfG4yQDByNk[5Oi=>
LY18 M1\4cmZ2dmO2aX;uJGF{e2G7 MVi0JO69VQ>? MY[xOkBp NELmcZNqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> Ml\VNVgxODZ4OU[=

... 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 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
Synonyms N/A

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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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID