R406

For research use only.

Catalog No.S2194

39 publications

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.

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Selleck's R406 has been cited by 39 publications

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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 NELXWIdHfW6ldHnvckBCe3OjeR?= NYnZdphFOSEQvF2= NX\y[m4zO8LiaB?= MXHy[YR2[2W|IH3p[5JifGmxbtMg MUCyOlI2OTd4MR?=
U266 M13XbWZ2dmO2aX;uJGF{e2G7 NHXyO3YyKM7:TR?= MoTVN:KhcA>? M{TEWZJm\HWlZYOgcYloemG2aX;uxsA> NXnB[Hh[OjZ{NUG3OlE>
Jeko-1 NUTHW|NGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX60PEBp Mn3CTWM2OD13LkC2PFI3KM7:TR?= Ml23NlU5OzV5NUW=
Mino NYj4TlF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkewOFghcA>? MnL0TWM2OD13LkewPFU1KM7:TR?= MnnzNlU5OzV5NUW=
Jeko-1 M1XDRmFxd3C2b4Ppd{BCe3OjeR?= MlKwOeKh|ryP MmHKNlQhcA>? MYnpcoR2[2W|IEK1MlHDqMLzwrCzMlLDqCViYYDvdJRwe2m| M3rXUFI2QDN3N{W1
primary MCL M3jFUGFxd3C2b4Ppd{BCe3OjeR?= M1XjVVIhyrWP NYDDbYpLOjRiaB?= NYLKR|BIcW6lcnXhd4V{KHOrZ37p[olk[W62bImgZZBweHSxc3nzxsA> NF:xNW0zPTN6OEO3Ny=>
PBMCs MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mor4NE02OCEQvF2= MoPiNlQhcA>? MXjEUXNQ MUnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M1TUS|I2OTJ5OE[y
PBMCs MWnGeY5kfGmxbjDBd5NigQ>? M4i1fFUh|ryP Mm\DNUBp NUT1SXQ6TE2VTx?= Mk\L[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> MWeyOVEzPzh4Mh?=
CFSE-CD4+ T  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjZZWU3OC5yNkK1MVEh|ryP MV:0JIQ> MXricI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? M2H6U|I1Pjd7OUiy
CFSE-CD11b+ NH7tdFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPt[GdkOC5yNkK1MVEh|ryP M{\IOVgh\A>? NHPXU2FjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= MWSyOFY4QTl6Mh?=
HMECs NILIOodHfW6ldHnvckBCe3OjeR?= NXHueHVLOC1zMDFOwG0> M{PweVIxKG2rbh?= NYLKcmdmcW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? NH[0WnQzPDN{OUW0OC=>
AB5 MXvBdI9xfG:|aYOgRZN{[Xl? M1rScFAuOi53IN88US=> M3GwPVQ5KGh? MlTYSG1UVw>? NVLQUZNRcW6mdXPld{BieG:ydH;zbZM> MnTINlM{QTh7MUG=
JB7 M1v0SmFxd3C2b4Ppd{BCe3OjeR?= M4jLfFAuOi53IN88US=> NInP[oU1QCCq M{T4NWROW09? M3W3Zolv\HWlZYOgZZBweHSxc3nz NVK3[3NTOjN|OUi5NVE>
AB5 NHTje3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTYNE0zNjVizszN NH7sXnc1QCCq NUPJcJhSTE2VTx?= NYDiblE1cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M1\uUFI{Ozl6OUGx
JB7 NX34NpR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHY[ncxNTJwNTFOwG0> MnvoOFghcA>? Ml;ZSG1UVw>? M3S2cYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NYC0cllYOjN|OUi5NVE>
RL NHnydY1HfW6ldHnvckBCe3OjeR?= NXTTT4p1Oi53L{Wg{txO NWXlTGpQOjRxNEigbC=> M3KyVmROW09? NHTWe49qdmS3Y3XzJIEheG:2ZX70JIRm[3KnYYPlJIlvKE2PUD25JI1TVkFiZYjwdoV{e2mxbh?= NHHnfYszOTl{Nkm2OS=>
RL M4DvVGZ2dmO2aX;uJGF{e2G7 MUexM|IvPSEQvF2= NHPLfFAzPCCq M2LmdGROW09? Mkj4doVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? MXSyNVkzPjl4NR?=
platelet  NV\IVVVzTnWwY4Tpc44hSXO|YYm= MmjiNeKh|ryv NIfKUFg2KG2rbh?= NY\aZ2FrcW6qaXLpeJMhTmQQs2LJTWEudWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25? NHy2Z4MzOTh2OE[5OC=>
platelet  M2nP[GZ2dmO2aX;uJGF{e2G7 NGLKfnMxNjB3L{GvNk42KM7:TR?= MV21JI1qdg>? Mo[zbY5pcWKrdIOgeIhmKHOrZ37hcIlv\yCvZXPoZY5qe22|IHTve45{fHKnYX2gc4YhTmQQs2LJTWE> M3PGRVIyQDR6Nkm0
DoHH2 MojQRZBweHSxc3nzJGF{e2G7 MnKzNE8{NzFyIN88US=> M37IeVQ5KGh? NXi4XmRFcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NFnIV5czODh5NUSwPC=>
Jeko-1  M2HCSWFxd3C2b4Ppd{BCe3OjeR?= NWe4UWdKOC9|L{GwJO69VQ>? MUe0PEBp NYDybVlWcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MYCyNFg4PTRyOB?=
Raji  NEmwcWJCeG:ydH;zbZMhSXO|YYm= NXLl[WtuOC9|L{GwJO69VQ>? MUO0PEBp NFT4[5RqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NEnBV|kzODh5NUSwPC=>
DHL4 M4nEWWFxd3C2b4Ppd{BCe3OjeR?= NV33b|luOC9zL{Sg{txO NEPvflM6PiCq MY\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MkTMNVgxODZ4OU[=
LY7 M4\KWGFxd3C2b4Ppd{BCe3OjeR?= MWWwM|EwPCEQvF2= MoXqPVYhcA>? NEO3emZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M1vxeVE5ODB4Nkm2
LY3 NWeyS2xbSXCxcITvd4l{KEG|c3H5 NGPWZ2ExNzFxNDFOwG0> M3zndFk3KGh? MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NGP0VmoyQDByNk[5Oi=>
DHL6 NUTzSnRQSXCxcITvd4l{KEG|c3H5 NGHsZXExNzFxNDFOwG0> NW\1WnlmQTZiaB?= NIXu[41qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MYSxPFAxPjZ7Nh?=
LY10 MnLYRZBweHSxc3nzJGF{e2G7 NF7zV5oxNzFxNDFOwG0> NETSZZU6PiCq NVvTcYF[cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MoGxNVgxODZ4OU[=
DHL10 M1O2ZWFxd3C2b4Ppd{BCe3OjeR?= NVW2WnZ3OC9zL{Sg{txO NV3WSlR2QTZiaB?= MYDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnnDNVgxODZ4OU[=
Wsu-NHL MV;BdI9xfG:|aYOgRZN{[Xl? NVX4SnU2OC9zL{Sg{txO MmLJPVYhcA>? MkDkbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MYGxPFAxPjZ7Nh?=
LY18 NF35XohCeG:ydH;zbZMhSXO|YYm= M{XwNFAwOS92IN88US=> MnfTPVYhcA>? NFPxfWNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Ml\4NVgxODZ4OU[=
LY1 MmTqRZBweHSxc3nzJGF{e2G7 MYqwM|EwPCEQvF2= MYC5OkBp NFjqN|dqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MWmxPFAxPjZ7Nh?=
DHL8 M4fGd2Fxd3C2b4Ppd{BCe3OjeR?= MoHnNE8yNzRizszN MnvoPVYhcA>? M37iSIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NYOxeGhtOThyME[2PVY>
DHL4 NXziZ2l1SXCxcITvd4l{KEG|c3H5 NE\vdY01KM7:TR?= MmLMPVYhcA>? NX\HUFNmcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? NILyT4gyQDByNk[5Oi=>
DHL6 MVHBdI9xfG:|aYOgRZN{[Xl? NEXXXZg1KM7:TR?= MYS5OkBp MV7pcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NGmycWQyQDByNk[5Oi=>
LY3 M1fXRmFxd3C2b4Ppd{BCe3OjeR?= NHG0[5M1KM7:TR?= NWDNfJFDQTZiaB?= NYPOe2U6cW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MUCxPFAxPjZ7Nh?=
LY7 MYrBdI9xfG:|aYOgRZN{[Xl? NVm5WnZlPCEQvF2= MX[5OkBp MXHpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 MmrDNVgxODZ4OU[=
DHL4 NY\1RoZnTnWwY4Tpc44hSXO|YYm= MUm0JO69VQ>? NE\lcokyPiCq NIjlcmdqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NIe4doMyQDByNk[5Oi=>
LY7 Mo\rSpVv[3Srb36gRZN{[Xl? MXS0JO69VQ>? NV70U5A1OTZiaB?= NHfENGNqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NGradWEyQDByNk[5Oi=>
LY3 NVnoO5ZWTnWwY4Tpc44hSXO|YYm= MVy0JO69VQ>? MVGxOkBp NInjN3NqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> M4K5SVE5ODB4Nkm2
DHL6 MXTGeY5kfGmxbjDBd5NigQ>? MXG0JO69VQ>? M4PINFE3KGh? MWrpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NWfZVpJXOThyME[2PVY>
LY10 NHfodJdHfW6ldHnvckBCe3OjeR?= MmW1OEDPxE1? NFvYOHMyPiCq M1HtOYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NUHYUVVDOThyME[2PVY>
Wsu-NHL Ml25SpVv[3Srb36gRZN{[Xl? NIDSWWg1KM7:TR?= NVr2RmhQOTZiaB?= NInH[ppqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> M4nYbVE5ODB4Nkm2
LY18 MWPGeY5kfGmxbjDBd5NigQ>? NHL5dHM1KM7:TR?= NVPSWJZHOTZiaB?= NYnodY5IcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NUe4dXI5OThyME[2PVY>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-RPS6 / T-RPS6 / p-4E-BP1 / T-4E-BP1; 

PubMed: 23535559     


Four AML cell lines (a and b) were treated for 24 hours with vehicle versus R406. Western blots of (a) p-RPS6 (Ser240/244) and (b) p-4E-BP1 (Thr37/46).

p-MEK / T-MEK / p-ERK / T-ERK; 

PubMed: 23535559     


AML cell lines were treated with vehicle versus R406. Western blots of p-MEK1/2 (Ser217/221) and p-ERK1/2 (Thr202/Tyr204) are depicted. 

p-c-RAF / T-c-RAF; 

PubMed: 23535559     


Effect of SYK inhibition on c-RAF in AML cells. AML cells were grown in the presence of 4 μM R406 for the indicated times and assessed for activation of c-RAF and ERK1/2.

p-AKT / T-AKT / p-mTOR / T-mTOR; 

PubMed: 23535559     


Western blot of (a) p-AKT (Ser473) or (b) p-mTOR (Ser2448) in AML cell lines treated with R406 for 24 hours.

23535559
Growth inhibition assay
Cell viability (U87, U251 cells); 

PubMed: 31043589     


U87 and U251 were insensitive to R406, with a calculated IC50 of more than 1 mM for both cell lines.

Cell viability (GSC lines); 

PubMed: 31043589     


Incubation with R406 significantly reduced the cell viability of both GSC lines, with an IC50 of 0.75 μM for GSC-1 and 0.89 μM for GSC-2 respectively. 

31043589
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]
- Collapse
  • Animal Models: Arthritis is induced in C57BL/6 mice by intraperitoneal injection of 150 μL of pooled sera from adult K/BxN mice.
  • 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(Data is from Selleck tests instead of citations):
5%dmso+95%cornoil
For best results, use promptly after mixing.
6mg/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
in solvent
Synonyms N/A
Smiles COC1=C(OC)C(=CC(=C1)NC2=NC(=C(F)C=N2)NC3=NC4=C(OC(C)(C)C(=O)N4)C=C3)OC.O[S](=O)(=O)C5=CC=CC=C5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01725230 Completed Drug: Fostamatinib|Drug: Rosuvastatin|Drug: Simvastatin Rheumatoid Arthritis AstraZeneca November 2012 Phase 1
NCT01598571 Completed Drug: Fostamatinib Healthy AstraZeneca May 2012 Phase 1
NCT01387308 Completed Drug: Fostamatinib Healthy AstraZeneca August 2011 Phase 1
NCT01355354 Completed Drug: Digoxin|Drug: Fostamatinib Healthy Volunteers|Rheumatoid Arthritis AstraZeneca June 2011 Phase 1

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