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 M{nXXGZ2dmO2aX;uJGF{e2G7 NUjldY9uOSEQvF2= M4i2SlPDqGh? M3jnTJJm\HWlZYOgcYloemG2aX;uxsA> NVi1V2dZOjZ{NUG3OlE>
U266 MUPGeY5kfGmxbjDBd5NigQ>? M{\BfFEh|ryP M3WyZlPDqGh? MW\y[YR2[2W|IH3p[5JifGmxbtMg MUWyOlI2OTd4MR?=
Jeko-1 NWXLcJZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvS[XBkPDhiaB?= NU\TT|RyUUN3ME21MlA3QDJ4IN88US=> NUDjSo9mOjV6M{W3OVU>
Mino NUH4d4tYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fTVVQ5KGh? MVXJR|UxRTVwN{C4OVQh|ryP NFjUUW4zPTh|NUe1OS=>
Jeko-1 NHHVd2xCeG:ydH;zbZMhSXO|YYm= NHfZfIQ2yqEQvF2= M2LRR|I1KGh? M1rV[4lv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= NVHzW|lkOjV6M{W3OVU>
primary MCL MUTBdI9xfG:|aYOgRZN{[Xl? M3u0NVIhyrWP MUWyOEBp NGDxNIdqdmO{ZXHz[ZMhe2mpbnnmbYNidnSueTDhdI9xfG:|aYRCpC=> MUmyOVM5QDN5Mx?=
PBMCs Mly3R4VtdCCYaXHibYxqfHliQYPzZZk> NX7Id|FnOC13MDFOwG0> MVuyOEBp NVrEb|FwTE2VTx?= MkDubY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NW\sZ3FtOjVzMke4OlI>
PBMCs NFy1XnVHfW6ldHnvckBCe3OjeR?= NF7mT482KM7:TR?= NVPL[2d3OSCq NF\wXnpFVVOR NYDQfWpZ\GWlcnXhd4V{KHSqZTDj[YxtKG2rZ4LheIlwdg>? NYLRU3lPOjVzMke4OlI>
CFSE-CD4+ T  NXHqbmtJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzKWW4xNjB4MkWtNUDPxE1? M3e0V|Qh\A>? NVT3ZYJX[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= Ml3YNlQ3Pzl7OEK=
CFSE-CD11b+ M4frUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrVR5QxNjB4MkWtNUDPxE1? MVW4JIQ> NXWzd3pO[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= MoX3NlQ3Pzl7OEK=
HMECs NVi0[5BuTnWwY4Tpc44hSXO|YYm= Mk\TNE0yOCEQvF2= M1fYN|IxKG2rbh?= NET5V4FqdmirYnn0d{BXTUeILYP0bY12dGG2ZXSgdoVt\WG|ZTDv[kBPVw>? NVzMeWZIOjR|Mkm1OFQ>
AB5 M{HXPGFxd3C2b4Ppd{BCe3OjeR?= MXiwMVIvPSEQvF2= MYW0PEBp Ml7JSG1UVw>? MVXpcoR2[2W|IHHwc5B1d3Orcx?= MUKyN|M6QDlzMR?=
JB7 NEPNOYhCeG:ydH;zbZMhSXO|YYm= MnLCNE0zNjVizszN NWHCe5N7PDhiaB?= MmXuSG1UVw>? NFGxfZdqdmS3Y3XzJIFxd3C2b4Ppdy=> MnvxNlM{QTh7MUG=
AB5 MoTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWwMVIvPSEQvF2= NY\DWHpbPDhiaB?= M2fuTGROW09? NUL1S4NRcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MXWyN|M6QDlzMR?=
JB7 NFjjVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXNc3gxNTJwNTFOwG0> NXLqTZNbPDhiaB?= MnLOSG1UVw>? M4PL[olv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NUDldlljOjN|OUi5NVE>
RL MUXGeY5kfGmxbjDBd5NigQ>? M4XqSVIvPS93IN88US=> MYiyOE81QCCq NGH6SW5FVVOR NEniTXZqdmS3Y3XzJIEheG:2ZX70JIRm[3KnYYPlJIlvKE2PUD25JI1TVkFiZYjwdoV{e2mxbh?= MlK5NlE6OjZ7NkW=
RL NFvFNZNHfW6ldHnvckBCe3OjeR?= NWnyZnc6OS9{LkWg{txO Mn3mNlQhcA>? NHzh[nFFVVOR MVzy[YR2[2W|IITo[UBi[3SrdnH0bY9vKG:oIFHreEBidmRicEewV|ZM MXuyNVkzPjl4NR?=
platelet  MULGeY5kfGmxbjDBd5NigQ>? Mo[5NeKh|ryv NVK4OldbPSCvaX6= NYXOfHRzcW6qaXLpeJMhTmQQs2LJTWEudWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25? M1jjfFIyQDR6Nkm0
platelet  MlXYSpVv[3Srb36gRZN{[Xl? M1jo[VAvODVxMT:yMlUh|ryP MYK1JI1qdg>? NWrpXG82cW6qaXLpeJMhfGinIIPp[45idGmwZzDt[YNp[W6rc33zJIRwf26|dILlZY0hd2ZiRnROt3JKUUF? NWDFfWliOjF6NEi2PVQ>
DoHH2 NWe0[GZFSXCxcITvd4l{KEG|c3H5 MWCwM|MwOTBizszN MWm0PEBp M2HLbYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NI\TcYszODh5NUSwPC=>
Jeko-1  M3zScWFxd3C2b4Ppd{BCe3OjeR?= NYPNU4Q{OC9|L{GwJO69VQ>? NFexeVg1QCCq MXTpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MV[yNFg4PTRyOB?=
Raji  MXXBdI9xfG:|aYOgRZN{[Xl? MnXDNE8{NzFyIN88US=> M3zDbVQ5KGh? NHrBNJdqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= MkfBNlA5PzV2MEi=
DHL4 MmG3RZBweHSxc3nzJGF{e2G7 MXWwM|EwPCEQvF2= MVm5OkBp Mo[0bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MmLSNVgxODZ4OU[=
LY7 MnvvRZBweHSxc3nzJGF{e2G7 NYTY[YJzOC9zL{Sg{txO M3rXfVk3KGh? M4rhXolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MUSxPFAxPjZ7Nh?=
LY3 Mnr2RZBweHSxc3nzJGF{e2G7 NYOzOJFWOC9zL{Sg{txO MYC5OkBp MXXpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M2fYelE5ODB4Nkm2
DHL6 M4LLZmFxd3C2b4Ppd{BCe3OjeR?= NXj3NGtGOC9zL{Sg{txO MnvpPVYhcA>? NWjzZmw{cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MYKxPFAxPjZ7Nh?=
LY10 M{LN[mFxd3C2b4Ppd{BCe3OjeR?= NV:zSHZ1OC9zL{Sg{txO M1\TV|k3KGh? MWrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnH4NVgxODZ4OU[=
DHL10 NV7q[GNmSXCxcITvd4l{KEG|c3H5 NV20[GF{OC9zL{Sg{txO NEDzOGw6PiCq NX\5fJpEcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MVexPFAxPjZ7Nh?=
Wsu-NHL M{LkemFxd3C2b4Ppd{BCe3OjeR?= MYSwM|EwPCEQvF2= Ml7kPVYhcA>? M1zUVolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1OwUlE5ODB4Nkm2
LY18 NYfUd4xrSXCxcITvd4l{KEG|c3H5 NH7YVVQxNzFxNDFOwG0> M2naS|k3KGh? NHPrenBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NGTPTXIyQDByNk[5Oi=>
LY1 MY\BdI9xfG:|aYOgRZN{[Xl? NHfPRWMxNzFxNDFOwG0> NWDYTpZKQTZiaB?= NGO5bXZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NXLhRm5NOThyME[2PVY>
DHL8 MnHhRZBweHSxc3nzJGF{e2G7 NWLBfHdnOC9zL{Sg{txO MmPxPVYhcA>? NHT5SpZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFrtbJgyQDByNk[5Oi=>
DHL4 M{HORWFxd3C2b4Ppd{BCe3OjeR?= NYq1PJdYPCEQvF2= MWe5OkBp MU\pcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MYixPFAxPjZ7Nh?=
DHL6 M4jKfmFxd3C2b4Ppd{BCe3OjeR?= M3jWUVQh|ryP MnzDPVYhcA>? MV7pcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MVmxPFAxPjZ7Nh?=
LY3 NUnoTJI6SXCxcITvd4l{KEG|c3H5 MkPJOEDPxE1? NFrrVpE6PiCq MkG4bY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MVmxPFAxPjZ7Nh?=
LY7 M4nFOWFxd3C2b4Ppd{BCe3OjeR?= NH7h[GI1KM7:TR?= NV;kcJZbQTZiaB?= NEfTclZqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MXKxPFAxPjZ7Nh?=
DHL4 NEXrTnJHfW6ldHnvckBCe3OjeR?= MknpOEDPxE1? MYmxOkBp MXvpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= M4TCXlE5ODB4Nkm2
LY7 MkTBSpVv[3Srb36gRZN{[Xl? MWW0JO69VQ>? Mn2zNVYhcA>? MUDpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NYrUc4VIOThyME[2PVY>
LY3 MYHGeY5kfGmxbjDBd5NigQ>? MVG0JO69VQ>? MW[xOkBp NXexe2VtcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MVexPFAxPjZ7Nh?=
DHL6 MlGySpVv[3Srb36gRZN{[Xl? NVmzV3BRPCEQvF2= M3PmPFE3KGh? NY[4dYRwcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MYKxPFAxPjZ7Nh?=
LY10 NYDFeJpUTnWwY4Tpc44hSXO|YYm= M1LwU|Qh|ryP M3nCS|E3KGh? NFWzdG9qdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MX2xPFAxPjZ7Nh?=
Wsu-NHL M2fxUmZ2dmO2aX;uJGF{e2G7 M3K1TFQh|ryP NXjHO3BLOTZiaB?= NV;He256cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NG\TfIUyQDByNk[5Oi=>
LY18 MVTGeY5kfGmxbjDBd5NigQ>? M3fyZVQh|ryP MVSxOkBp MXjpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NEnV[nYyQDByNk[5Oi=>

... 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.

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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