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 NGfqSpZHfW6ldHnvckBCe3OjeR?= NHvMOlcyKM7:TR?= NX\SPFBsO8LiaB?= NEHYclBz\WS3Y3XzJI1q\3KjdHnvcuKh M4DiV|I3OjVzN{[x
U266 NU\nWG5WTnWwY4Tpc44hSXO|YYm= NX\TdpBNOSEQvF2= NIT1dnk{yqCq NUjrWXVqemWmdXPld{BucWe{YYTpc47DqA>? NWPGSmF2OjZ{NUG3OlE>
Jeko-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HWNFQ5KGh? NHfXfnlKSzVyPUWuNFY5OjZizszN NEfyPYszPTh|NUe1OS=>
Mino MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXW0PEBp NILxbZRKSzVyPUWuO|A5PTRizszN NHHVb40zPTh|NUe1OS=>
Jeko-1 NIrtcZdCeG:ydH;zbZMhSXO|YYm= MnnzOeKh|ryP NULiW|JyOjRiaB?= NEDGZo1qdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz M4nOOFI2QDN3N{W1
primary MCL NVTwRm5QSXCxcITvd4l{KEG|c3H5 NV7LboNCOiEEtV2= NWrSPW1rOjRiaB?= M3e5UYlv[3KnYYPld{B{cWewaX\pZ4FvfGy7IHHwc5B1d3Orc9Mg MmGyNlU{QDh|N{O=
PBMCs NXftT4NMS2WubDDWbYFjcWyrdImgRZN{[Xl? NH64NGQxNTVyIN88US=> MmizNlQhcA>? NHjtNpZFVVOR MXfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXXzXpRCOjVzMke4OlI>
PBMCs M17mfmZ2dmO2aX;uJGF{e2G7 NIfOeoM2KM7:TR?= Mm\xNUBp M3G0TWROW09? MkHo[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> NYfZ[FNZOjVzMke4OlI>
CFSE-CD4+ T  MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LXR|AvODZ{NT2xJO69VQ>? M4jZS|Qh\A>? MYHicI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? NU\wWWd1OjR4N{m5PFI>
CFSE-CD11b+ NHTxcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjFb5V7OC5yNkK1MVEh|ryP MkjYPEBl MX\icI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? MnnzNlQ3Pzl7OEK=
HMECs NYqwNm1FTnWwY4Tpc44hSXO|YYm= MVKwMVExKM7:TR?= NV\qblNUOjBibXnu MVTpcohq[mm2czDWSWdHNXO2aX31cIF1\WRicnXs[YF{\SCxZjDOUy=> NVi1fG5rOjR|Mkm1OFQ>
AB5 NHH6eYlCeG:ydH;zbZMhSXO|YYm= MVGwMVIvPSEQvF2= MkX6OFghcA>? MX;EUXNQ MXnpcoR2[2W|IHHwc5B1d3Orcx?= NHj5[XYzOzN7OEmxNS=>
JB7 MWrBdI9xfG:|aYOgRZN{[Xl? NFXF[HkxNTJwNTFOwG0> NYfxWZNJPDhiaB?= MmHiSG1UVw>? M{H5WIlv\HWlZYOgZZBweHSxc3nz NHu2RoszOzN7OEmxNS=>
AB5 Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln5NE0zNjVizszN M2\EPVQ5KGh? MlziSG1UVw>? NYfJVpY{cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NGG1Z4IzOzN7OEmxNS=>
JB7 NIP3e4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fEU|AuOi53IN88US=> MXy0PEBp MU\EUXNQ NVH5Z2FQcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NUmwZmVEOjN|OUi5NVE>
RL NWHibItYTnWwY4Tpc44hSXO|YYm= MoX4Nk42NzVizszN NGTneFMzPC92ODDo M1zVOGROW09? NH73U2VqdmS3Y3XzJIEheG:2ZX70JIRm[3KnYYPlJIlvKE2PUD25JI1TVkFiZYjwdoV{e2mxbh?= M{S2NVIyQTJ4OU[1
RL MofqSpVv[3Srb36gRZN{[Xl? Ml21NU8zNjVizszN NIqwWmEzPCCq MlLZSG1UVw>? NVjjNlduemWmdXPld{B1cGViYXP0bZZifGmxbjDv[kBCc3RiYX7kJJA4OFN4Sx?= M2TWSlIyQTJ4OU[1
platelet  MY\GeY5kfGmxbjDBd5NigQ>? M3XzeVHDqM7:bR?= M33PZ|UhdWmw M3S5W4lvcGmkaYTzJGZk|rOUSVnBMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9v MU[yNVg1QDZ7NB?=
platelet  NEG4[W1HfW6ldHnvckBCe3OjeR?= M4G5PVAvODVxMT:yMlUh|ryP NGHrclI2KG2rbh?= NH7GSGtqdmirYnn0d{B1cGVic3nncoFtcW6pIH3lZ4hidmm|bYOg[I94dnO2cnXhcUBw\iCIY98zVmlKSQ>? MXSyNVg1QDZ7NB?=
DoHH2 M3fnTmFxd3C2b4Ppd{BCe3OjeR?= NUThcHZtOC9|L{GwJO69VQ>? NV;ONWNKPDhiaB?= NV\1b2w{cW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NETUNnkzODh5NUSwPC=>
Jeko-1  NGXnZpVCeG:ydH;zbZMhSXO|YYm= NGfZfHExNzNxMUCg{txO NY[2WHJjPDhiaB?= MUTpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? NXfCSphiOjB6N{W0NFg>
Raji  NV:xO2tYSXCxcITvd4l{KEG|c3H5 NWXFOYJvOC9|L{GwJO69VQ>? NHvpO5E1QCCq M3HLeolv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 MWGyNFg4PTRyOB?=
DHL4 M1uzUWFxd3C2b4Ppd{BCe3OjeR?= MYSwM|EwPCEQvF2= NY\3O2o5QTZiaB?= MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MUOxPFAxPjZ7Nh?=
LY7 Mn73RZBweHSxc3nzJGF{e2G7 MVKwM|EwPCEQvF2= MVK5OkBp M4jFN4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= Ml76NVgxODZ4OU[=
LY3 M2nRZ2Fxd3C2b4Ppd{BCe3OjeR?= M37ke|AwOS92IN88US=> M{\oO|k3KGh? MVHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MVuxPFAxPjZ7Nh?=
DHL6 MYjBdI9xfG:|aYOgRZN{[Xl? M4T3XlAwOS92IN88US=> NVnqR3FtQTZiaB?= MVHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M1\xWlE5ODB4Nkm2
LY10 MYXBdI9xfG:|aYOgRZN{[Xl? Mn;oNE8yNzRizszN M{nEfFk3KGh? NXP2fWJrcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MmPINVgxODZ4OU[=
DHL10 NYLYTJg3SXCxcITvd4l{KEG|c3H5 M4ToUFAwOS92IN88US=> NW\CNmJCQTZiaB?= MkDMbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M135bFE5ODB4Nkm2
Wsu-NHL M2j2cGFxd3C2b4Ppd{BCe3OjeR?= NXu2PHZWOC9zL{Sg{txO MUi5OkBp NHTyRYZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFKwOmMyQDByNk[5Oi=>
LY18 MXTBdI9xfG:|aYOgRZN{[Xl? MXSwM|EwPCEQvF2= M3\oNFk3KGh? NUHmbGhMcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NEXMRoUyQDByNk[5Oi=>
LY1 MnWzRZBweHSxc3nzJGF{e2G7 NEfCbFYxNzFxNDFOwG0> M3K0Nlk3KGh? MUHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M{XJSFE5ODB4Nkm2
DHL8 NUDEWJFSSXCxcITvd4l{KEG|c3H5 Mn;PNE8yNzRizszN M3PSSVk3KGh? M3HyeIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MV6xPFAxPjZ7Nh?=
DHL4 NXLLR45{SXCxcITvd4l{KEG|c3H5 M4XjZlQh|ryP M3O0VVk3KGh? NFy5NZJqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NHHmOoMyQDByNk[5Oi=>
DHL6 MnjFRZBweHSxc3nzJGF{e2G7 NH3xeFk1KM7:TR?= M3\KR|k3KGh? MnLKbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MX6xPFAxPjZ7Nh?=
LY3 NGW3UIVCeG:ydH;zbZMhSXO|YYm= M3nxV|Qh|ryP NEjzXWo6PiCq MWjpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MmDwNVgxODZ4OU[=
LY7 MWfBdI9xfG:|aYOgRZN{[Xl? M{nRZVQh|ryP Mn;5PVYhcA>? NGW4VHRqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NEm5XlQyQDByNk[5Oi=>
DHL4 MWPGeY5kfGmxbjDBd5NigQ>? MV20JO69VQ>? M4DaXFE3KGh? Ml\SbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NWWxN2J6OThyME[2PVY>
LY7 Mo\WSpVv[3Srb36gRZN{[Xl? NImxPI01KM7:TR?= MonBNVYhcA>? M1T4XolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NHrJT5EyQDByNk[5Oi=>
LY3 M3fRSWZ2dmO2aX;uJGF{e2G7 MUG0JO69VQ>? MUmxOkBp MVfpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MYKxPFAxPjZ7Nh?=
DHL6 NYDTV|A{TnWwY4Tpc44hSXO|YYm= M{XtTlQh|ryP MUCxOkBp NF;nd|ZqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NWnnWFBiOThyME[2PVY>
LY10 MoDPSpVv[3Srb36gRZN{[Xl? MYG0JO69VQ>? MYOxOkBp MmPxbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MmPQNVgxODZ4OU[=
Wsu-NHL MXrGeY5kfGmxbjDBd5NigQ>? MYS0JO69VQ>? NE\ZVVQyPiCq M1n1cYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MVqxPFAxPjZ7Nh?=
LY18 M{fYfGZ2dmO2aX;uJGF{e2G7 M4D4TFQh|ryP NV7qNGJbOTZiaB?= NWPWe4s5cW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NVfXb3pzOThyME[2PVY>

... 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
+ 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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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.

Syk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID