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 MlzUSpVv[3Srb36gRZN{[Xl? NYDMTWg4OSEQvF2= NFHRRno{yqCq NYL6T216emWmdXPld{BucWe{YYTpc47DqA>? MnvUNlYzPTF5NkG=
U266 NHvLcXhHfW6ldHnvckBCe3OjeR?= NHTrTYYyKM7:TR?= NXzlU|hZO8LiaB?= M{nHd5Jm\HWlZYOgcYloemG2aX;uxsA> MWmyOlI2OTd4MR?=
Jeko-1 NEjDNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HoTFQ5KGh? Mm\PTWM2OD13LkC2PFI3KM7:TR?= NEOwNVUzPTh|NUe1OS=>
Mino M1z3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[0PEBp MmjOTWM2OD13LkewPFU1KM7:TR?= M1TrU|I2QDN3N{W1
Jeko-1 NVjUR2NKSXCxcITvd4l{KEG|c3H5 MVK1xsDPxE1? NInqR2UzPCCq MWHpcoR2[2W|IEK1MlHDqMLzwrCzMlLDqCViYYDvdJRwe2m| M2rVO|I2QDN3N{W1
primary MCL MWLBdI9xfG:|aYOgRZN{[Xl? M4T0TlIhyrWP M4LvcVI1KGh? NYPoXnE2cW6lcnXhd4V{KHOrZ37p[olk[W62bImgZZBweHSxc3nzxsA> MUmyOVM5QDN5Mx?=
PBMCs MmfhR4VtdCCYaXHibYxqfHliQYPzZZk> MXqwMVUxKM7:TR?= MofWNlQhcA>? NVLLdI9kTE2VTx?= M{PifYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mm\ENlUyOjd6NkK=
PBMCs NWPqW45WTnWwY4Tpc44hSXO|YYm= M4jkRlUh|ryP MWSxJIg> M3HNS2ROW09? MWTk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u NYTCeHVGOjVzMke4OlI>
CFSE-CD4+ T  NU\sU|R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDvZnoxNjB4MkWtNUDPxE1? M{LTelQh\A>? NYe3fWZI[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= M1jlU|I1Pjd7OUiy
CFSE-CD11b+ M2OySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGwMlA3OjVvMTFOwG0> MmnjPEBl NVLrZlJY[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= NHT6e4EzPDZ5OUm4Ni=>
HMECs MYDGeY5kfGmxbjDBd5NigQ>? M4CySlAuOTBizszN M4jET|IxKG2rbh?= MVXpcohq[mm2czDWSWdHNXO2aX31cIF1\WRicnXs[YF{\SCxZjDOUy=> MnzTNlQ{Ojl3NES=
AB5 MnLNRZBweHSxc3nzJGF{e2G7 NITGbXYxNTJwNTFOwG0> MXS0PEBp MlrpSG1UVw>? MU\pcoR2[2W|IHHwc5B1d3Orcx?= MYWyN|M6QDlzMR?=
JB7 NYDqPGNzSXCxcITvd4l{KEG|c3H5 NHzjUnYxNTJwNTFOwG0> MYi0PEBp M2[4UWROW09? M2LseIlv\HWlZYOgZZBweHSxc3nz MXuyN|M6QDlzMR?=
AB5 MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmye4IxNTJwNTFOwG0> MX[0PEBp NVnP[mNETE2VTx?= MljWbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MnHlNlM{QTh7MUG=
JB7 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILEVnQxNTJwNTFOwG0> M2q4bFQ5KGh? MV\EUXNQ NVLJNIVncW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MUGyN|M6QDlzMR?=
RL Mn:3SpVv[3Srb36gRZN{[Xl? M4XZNFIvPS93IN88US=> MVqyOE81QCCq NXTadIZ4TE2VTx?= MojobY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? MVOyNVkzPjl4NR?=
RL M1S2WmZ2dmO2aX;uJGF{e2G7 NX\tclVXOS9{LkWg{txO M2\xRlI1KGh? NEnXeHlFVVOR MWPy[YR2[2W|IITo[UBi[3SrdnH0bY9vKG:oIFHreEBidmRicEewV|ZM MonmNlE6OjZ7NkW=
platelet  NH31[HlHfW6ldHnvckBCe3OjeR?= NXjaWpRHOcLizszt MmGwOUBucW5? M{TqcIlvcGmkaYTzJGZk|rOUSVnBMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9v NV22OFVuOjF6NEi2PVQ>
platelet  MYnGeY5kfGmxbjDBd5NigQ>? Mlf0NE4xPS9zL{KuOUDPxE1? MVW1JI1qdg>? MULpcohq[mm2czD0bIUhe2mpbnHsbY5oKG2nY3jhcol{dXNiZH;3cpN1emWjbTDv[kBH[87|UlnJRS=> NIK2NW4zOTh2OE[5OC=>
DoHH2 NW\xc2QzSXCxcITvd4l{KEG|c3H5 M1L4eVAwOy9zMDFOwG0> NID2WoQ1QCCq NU\iRlJTcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MoLFNlA5PzV2MEi=
Jeko-1  MVvBdI9xfG:|aYOgRZN{[Xl? MkOxNE8{NzFyIN88US=> M1Hkd|Q5KGh? Ml2xbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? NVzUVmt7OjB6N{W0NFg>
Raji  MVzBdI9xfG:|aYOgRZN{[Xl? MYWwM|MwOTBizszN MYm0PEBp NHXPdpRqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= M4G4PFIxQDd3NEC4
DHL4 MV\BdI9xfG:|aYOgRZN{[Xl? NH;yWWkxNzFxNDFOwG0> NFfhXZI6PiCq NFvhfYxqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NYD5bZNMOThyME[2PVY>
LY7 MUfBdI9xfG:|aYOgRZN{[Xl? NG\Z[mIxNzFxNDFOwG0> NHPjTWw6PiCq NHfMTFdqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M1;aO|E5ODB4Nkm2
LY3 M3PjNWFxd3C2b4Ppd{BCe3OjeR?= NWmwbpRbOC9zL{Sg{txO MnnXPVYhcA>? NXL3U4JQcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NWfXUphJOThyME[2PVY>
DHL6 MYPBdI9xfG:|aYOgRZN{[Xl? M4nwflAwOS92IN88US=> MYW5OkBp Mln4bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NEjRcGUyQDByNk[5Oi=>
LY10 NETnUo5CeG:ydH;zbZMhSXO|YYm= MXSwM|EwPCEQvF2= MmPUPVYhcA>? NEO1[VlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVHRNZFxOThyME[2PVY>
DHL10 NFzSTYFCeG:ydH;zbZMhSXO|YYm= NFrxXY0xNzFxNDFOwG0> NHXTd3o6PiCq MWjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 Mn;YNVgxODZ4OU[=
Wsu-NHL MU\BdI9xfG:|aYOgRZN{[Xl? M3v2R|AwOS92IN88US=> MUm5OkBp M2XNUIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Mn;NNVgxODZ4OU[=
LY18 NXTWcGVUSXCxcITvd4l{KEG|c3H5 M3q1[|AwOS92IN88US=> MX[5OkBp Mni2bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M{HHflE5ODB4Nkm2
LY1 NFizZ5JCeG:ydH;zbZMhSXO|YYm= MlzONE8yNzRizszN M1\kOlk3KGh? NFjjOZFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MlTFNVgxODZ4OU[=
DHL8 NX7mOY9YSXCxcITvd4l{KEG|c3H5 NYP1R2R4OC9zL{Sg{txO MnvoPVYhcA>? MWrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MonUNVgxODZ4OU[=
DHL4 NH;KNmdCeG:ydH;zbZMhSXO|YYm= M{\Oe|Qh|ryP NEHHUWo6PiCq M4\jU4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NGe1cGsyQDByNk[5Oi=>
DHL6 NHXjWnlCeG:ydH;zbZMhSXO|YYm= NVjXTXdpPCEQvF2= MUK5OkBp M4HMeIlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MlLWNVgxODZ4OU[=
LY3 NXHsbVZnSXCxcITvd4l{KEG|c3H5 NIXZUIk1KM7:TR?= MYG5OkBp MVnpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NUGzRYc6OThyME[2PVY>
LY7 NEj6dVhCeG:ydH;zbZMhSXO|YYm= MkfiOEDPxE1? M2n2VVk3KGh? MXLpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NGe2WXMyQDByNk[5Oi=>
DHL4 NV\qc2RnTnWwY4Tpc44hSXO|YYm= MUW0JO69VQ>? M{C2TVE3KGh? NGLjVoVqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MmrmNVgxODZ4OU[=
LY7 NFm3RWdHfW6ldHnvckBCe3OjeR?= NHvVeXI1KM7:TR?= MnrhNVYhcA>? MlfGbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MlW1NVgxODZ4OU[=
LY3 NXjQ[4w2TnWwY4Tpc44hSXO|YYm= NEKyfGY1KM7:TR?= NWHl[4d{OTZiaB?= NUC1PVlpcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MVmxPFAxPjZ7Nh?=
DHL6 NF3WUZJHfW6ldHnvckBCe3OjeR?= M{PPXlQh|ryP NILvbY4yPiCq NEH6UmdqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NFfWb|kyQDByNk[5Oi=>
LY10 NXXQb5h4TnWwY4Tpc44hSXO|YYm= NFHDUo01KM7:TR?= MYqxOkBp NHPjWoNqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NFG2dnMyQDByNk[5Oi=>
Wsu-NHL M4rzTGZ2dmO2aX;uJGF{e2G7 M{flXVQh|ryP MYSxOkBp NGCwUIpqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MXyxPFAxPjZ7Nh?=
LY18 NH\1cZhHfW6ldHnvckBCe3OjeR?= MX:0JO69VQ>? NWmyTIU5OTZiaB?= NHfnZYRqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MVmxPFAxPjZ7Nh?=

... 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 to the product individually and in order:
30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.
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.

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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