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 NVnMT2d1TnWwY4Tpc44hSXO|YYm= NEf5[G4yKM7:TR?= NV3VVIlXO8LiaB?= NFPRNHhz\WS3Y3XzJI1q\3KjdHnvcuKh NV:1epZ2OjZ{NUG3OlE>
U266 NUH1NVVmTnWwY4Tpc44hSXO|YYm= NWW4S|M{OSEQvF2= NGf5c5c{yqCq Mn;adoVlfWOnczDtbYdz[XSrb39CpC=> NWnqOFFPOjZ{NUG3OlE>
Jeko-1 NXj3W3Y3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;lOFghcA>? NETDb3dKSzVyPUWuNFY5OjZizszN MliwNlU5OzV5NUW=
Mino NGLYU3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M12xV|Q5KGh? MWXJR|UxRTVwN{C4OVQh|ryP NHrTfmUzPTh|NUe1OS=>
Jeko-1 MYLBdI9xfG:|aYOgRZN{[Xl? M3q5fVXDqM7:TR?= M1zUWVI1KGh? NVG5SGM6cW6mdXPld{AzPS5zwrFCteKhOy5{wrClJIFxd3C2b4Ppdy=> M33mRlI2QDN3N{W1
primary MCL M32wPGFxd3C2b4Ppd{BCe3OjeR?= NE\G[JQzKML3TR?= MWCyOEBp NGrwOFdqdmO{ZXHz[ZMhe2mpbnnmbYNidnSueTDhdI9xfG:|aYRCpC=> MV:yOVM5QDN5Mx?=
PBMCs NUC3e3h{S2WubDDWbYFjcWyrdImgRZN{[Xl? MVuwMVUxKM7:TR?= MWGyOEBp MXjEUXNQ NXqyPHVCcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmW2NlUyOjd6NkK=
PBMCs NWO3[5lDTnWwY4Tpc44hSXO|YYm= NF7hT|M2KM7:TR?= NY\4T5ZqOSCq NU[1bVk6TE2VTx?= NHfkWlRl\WO{ZXHz[ZMhfGinIHPlcIwhdWmpcnH0bY9v NIXaZYIzPTF{N{i2Ni=>
CFSE-CD4+ T  NXrHcIV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKwMlA3OjVvMTFOwG0> NXzYbmRCPCCm M3rBSYJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| MXKyOFY4QTl6Mh?=
CFSE-CD11b+ MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvtTo5JOC5yNkK1MVEh|ryP NHLKTIk5KGR? Mkm4Zoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? MmLJNlQ3Pzl7OEK=
HMECs M4Xu[mZ2dmO2aX;uJGF{e2G7 NIf4eGQxNTFyIN88US=> MmDvNlAhdWmw Mo\rbY5pcWKrdIOgWmVITi2|dHnteYxifGWmIILlcIVie2Vib3[gUm8> MV:yOFMzQTV2NB?=
AB5 M3K3TmFxd3C2b4Ppd{BCe3OjeR?= M3i4fFAuOi53IN88US=> Mn3zOFghcA>? M3fKeWROW09? M4DCT4lv\HWlZYOgZZBweHSxc3nz M2XkclI{Ozl6OUGx
JB7 MnjIRZBweHSxc3nzJGF{e2G7 NFrSXIwxNTJwNTFOwG0> MkLPOFghcA>? MmjTSG1UVw>? MUjpcoR2[2W|IHHwc5B1d3Orcx?= Mlf4NlM{QTh7MUG=
AB5 NWXoWlhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2wMVIvPSEQvF2= Ml;aOFghcA>? M4K3PGROW09? NVvTSnRscW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NXmxflNqOjN|OUi5NVE>
JB7 NUC5ZZlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPrNE0zNjVizszN MWK0PEBp NXfFZ3lQTE2VTx?= MUDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MnmxNlM{QTh7MUG=
RL NH74ZlZHfW6ldHnvckBCe3OjeR?= MlLCNk42NzVizszN NV\GenJvOjRxNEigbC=> MVzEUXNQ MYLpcoR2[2W|IHGgdI91\W62IHTlZ5Jm[XOnIHnuJG1OWC17IH3SUmEh\XiycnXzd4lwdg>? MoHrNlE6OjZ7NkW=
RL M{jp[mZ2dmO2aX;uJGF{e2G7 NUfSZ3VXOS9{LkWg{txO MWOyOEBp NF7tfVRFVVOR MXry[YR2[2W|IITo[UBi[3SrdnH0bY9vKG:oIFHreEBidmRicEewV|ZM NH7IZmgzOTl{Nkm2OS=>
platelet  M2Swe2Z2dmO2aX;uJGF{e2G7 NU\BU2dvOcLizszt MkDoOUBucW5? NYTMdopOcW6qaXLpeJMhTmQQs2LJTWEudWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25? M4KyRlIyQDR6Nkm0
platelet  MXTGeY5kfGmxbjDBd5NigQ>? NILoXHcxNjB3L{GvNk42KM7:TR?= NE[3[2Q2KG2rbh?= MknjbY5pcWKrdIOgeIhmKHOrZ37hcIlv\yCvZXPoZY5qe22|IHTve45{fHKnYX2gc4YhTmQQs2LJTWE> NWXBdpduOjF6NEi2PVQ>
DoHH2 MoHZRZBweHSxc3nzJGF{e2G7 NWDYSpVHOC9|L{GwJO69VQ>? NEf1RoM1QCCq MVrpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MoLiNlA5PzV2MEi=
Jeko-1  MmXwRZBweHSxc3nzJGF{e2G7 NGG2XmQxNzNxMUCg{txO NV3rOWZvPDhiaB?= NFfJS2RqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NV;QVFBNOjB6N{W0NFg>
Raji  M{HSUmFxd3C2b4Ppd{BCe3OjeR?= MnPZNE8{NzFyIN88US=> M3TjdVQ5KGh? NF7zdJlqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NXvWWGtJOjB6N{W0NFg>
DHL4 NUfVc|hoSXCxcITvd4l{KEG|c3H5 NUS1cFhVOC9zL{Sg{txO M2Pjblk3KGh? MkPFbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NEHR[o0yQDByNk[5Oi=>
LY7 NXn1c|JpSXCxcITvd4l{KEG|c3H5 M4fQTFAwOS92IN88US=> NYC1dm45QTZiaB?= M3\3S4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1Xie|E5ODB4Nkm2
LY3 M3nzS2Fxd3C2b4Ppd{BCe3OjeR?= MUWwM|EwPCEQvF2= MXO5OkBp NG\ES|RqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NGrFbFkyQDByNk[5Oi=>
DHL6 Ml7FRZBweHSxc3nzJGF{e2G7 Mk[xNE8yNzRizszN M1LPTVk3KGh? MWXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MVmxPFAxPjZ7Nh?=
LY10 NGnMVXpCeG:ydH;zbZMhSXO|YYm= NWnifW5QOC9zL{Sg{txO NHewR4s6PiCq MWLpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M4fqdVE5ODB4Nkm2
DHL10 MniwRZBweHSxc3nzJGF{e2G7 NF\5PYYxNzFxNDFOwG0> M4fEdlk3KGh? NXrIXml{cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M{LH[|E5ODB4Nkm2
Wsu-NHL NFmwcHZCeG:ydH;zbZMhSXO|YYm= M1TjVlAwOS92IN88US=> MYS5OkBp NFXPeY5qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MVSxPFAxPjZ7Nh?=
LY18 Ml7uRZBweHSxc3nzJGF{e2G7 M2rXO|AwOS92IN88US=> NFnrPXI6PiCq MWrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MmDnNVgxODZ4OU[=
LY1 Mk\0RZBweHSxc3nzJGF{e2G7 M1P5b|AwOS92IN88US=> MlG2PVYhcA>? MkTobY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MWmxPFAxPjZ7Nh?=
DHL8 MnfRRZBweHSxc3nzJGF{e2G7 NHjlfpkxNzFxNDFOwG0> MknTPVYhcA>? NGXGWlRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NXLr[nIyOThyME[2PVY>
DHL4 M4TuTmFxd3C2b4Ppd{BCe3OjeR?= NVPWdVVYPCEQvF2= M{jK[lk3KGh? MVzpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MVGxPFAxPjZ7Nh?=
DHL6 MUDBdI9xfG:|aYOgRZN{[Xl? NVLKNWRzPCEQvF2= NYe2enNFQTZiaB?= MoHobY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> NUDnOIpEOThyME[2PVY>
LY3 M1vr[mFxd3C2b4Ppd{BCe3OjeR?= MUC0JO69VQ>? NFy0O4w6PiCq NUOw[5R[cW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? M1LHNFE5ODB4Nkm2
LY7 M2HpfWFxd3C2b4Ppd{BCe3OjeR?= M1G0[lQh|ryP NWXjXZE5QTZiaB?= M2PSNIlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MW[xPFAxPjZ7Nh?=
DHL4 MWTGeY5kfGmxbjDBd5NigQ>? MWe0JO69VQ>? M1q2NlE3KGh? NVXCVot{cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> M{TofVE5ODB4Nkm2
LY7 MXXGeY5kfGmxbjDBd5NigQ>? MVS0JO69VQ>? M33PSFE3KGh? MojybY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NYPG[m1jOThyME[2PVY>
LY3 Mmi0SpVv[3Srb36gRZN{[Xl? NF34SoE1KM7:TR?= MmrJNVYhcA>? MWLpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= Mk\jNVgxODZ4OU[=
DHL6 MoPXSpVv[3Srb36gRZN{[Xl? NIfqXVI1KM7:TR?= MlTkNVYhcA>? NWC3U3lQcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MnXzNVgxODZ4OU[=
LY10 MlqxSpVv[3Srb36gRZN{[Xl? MWC0JO69VQ>? MnPUNVYhcA>? M33hdolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M2DFTlE5ODB4Nkm2
Wsu-NHL NH;CPJlHfW6ldHnvckBCe3OjeR?= NFzlN|g1KM7:TR?= MoDBNVYhcA>? MXvpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MUGxPFAxPjZ7Nh?=
LY18 NUP2O5ZFTnWwY4Tpc44hSXO|YYm= MVm0JO69VQ>? MkLYNVYhcA>? M2TqNIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MmPVNVgxODZ4OU[=

... 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
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