R406

For research use only.

Catalog No.S2194

39 publications

R406 Chemical Structure

CAS No. 841290-81-1

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. R406 induces apoptosis. 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. R406 induces apoptosis. 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 M3\WXGZ2dmO2aX;uJGF{e2G7 MY[xJO69VQ>? MnjoN:KhcA>? MljldoVlfWOnczDtbYdz[XSrb39CpC=> NFTRfIozPjJ3MUe2NS=>
U266 NGW4NXRHfW6ldHnvckBCe3OjeR?= MYKxJO69VQ>? NIfsPGM{yqCq M2HTU5Jm\HWlZYOgcYloemG2aX;uxsA> M1f0[VI3OjVzN{[x
Jeko-1 MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXq0PEBp MnP0TWM2OD13LkC2PFI3KM7:TR?= M4DxeFI2QDN3N{W1
Mino Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3afXQ1QCCq M2OwO2lEPTB;NT63NFg2PCEQvF2= MXyyOVg{PTd3NR?=
Jeko-1 M1\XdmFxd3C2b4Ppd{BCe3OjeR?= NFfvdJY2yqEQvF2= MmXNNlQhcA>? MmrtbY5lfWOnczCyOU4yyqEEsdMgN{4zyqBnIHHwc5B1d3Orcx?= MmPuNlU5OzV5NUW=
primary MCL M3rMWmFxd3C2b4Ppd{BCe3OjeR?= MlnmNkDDvU1? NUfMWYdxOjRiaB?= NXPkeYxMcW6lcnXhd4V{KHOrZ37p[olk[W62bImgZZBweHSxc3nzxsA> MlTQNlU{QDh|N{O=
PBMCs MnjHR4VtdCCYaXHibYxqfHliQYPzZZk> NF7TNo8xNTVyIN88US=> NXHXO5A6OjRiaB?= MkPBSG1UVw>? MmPLbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUPYWoIxOjVzMke4OlI>
PBMCs NFHXSo1HfW6ldHnvckBCe3OjeR?= MmniOUDPxE1? MVGxJIg> NFuydYNFVVOR M4q3ZoRm[3KnYYPld{B1cGViY3XscEBucWe{YYTpc44> M33yVlI2OTJ5OE[y
CFSE-CD4+ T  NWjYepJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWKwMlA3OjVvMTFOwG0> NUTLSmtrPCCm NXvIdmRQ[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= MlPHNlQ3Pzl7OEK=
CFSE-CD11b+ NVO4TVFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSwMlA3OjVvMTFOwG0> NFrqfYU5KGR? M4LuW4Jtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| M3LDcFI1Pjd7OUiy
HMECs Ml;tSpVv[3Srb36gRZN{[Xl? MlzWNE0yOCEQvF2= Mk\INlAhdWmw Mnv0bY5pcWKrdIOgWmVITi2|dHnteYxifGWmIILlcIVie2Vib3[gUm8> NUXYbW8{OjR|Mkm1OFQ>
AB5 NXLHNm5OSXCxcITvd4l{KEG|c3H5 NWS2VIUxOC1{LkWg{txO NHPHfVg1QCCq NILFV2NFVVOR MYfpcoR2[2W|IHHwc5B1d3Orcx?= NF3TZ2YzOzN7OEmxNS=>
JB7 M{PzOWFxd3C2b4Ppd{BCe3OjeR?= NI\Peo4xNTJwNTFOwG0> MXW0PEBp MkPoSG1UVw>? MoHQbY5lfWOnczDhdI9xfG:|aYO= MWGyN|M6QDlzMR?=
AB5 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjoNE0zNjVizszN NVv4[md5PDhiaB?= NHjGVGxFVVOR MX7pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NYrud4diOjN|OUi5NVE>
JB7 MlXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm3[5ZrOC1{LkWg{txO MmWwOFghcA>? M1zzb2ROW09? M3\WT4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Ml3INlM{QTh7MUG=
RL MmPnSpVv[3Srb36gRZN{[Xl? M{[1[lIvPS93IN88US=> MXmyOE81QCCq M373cGROW09? Mn;2bY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? NHXzU2QzOTl{Nkm2OS=>
RL M1L3cGZ2dmO2aX;uJGF{e2G7 MUWxM|IvPSEQvF2= NYDmcWY4OjRiaB?= MW\EUXNQ MXny[YR2[2W|IITo[UBi[3SrdnH0bY9vKG:oIFHreEBidmRicEewV|ZM M2XuSFIyQTJ4OU[1
platelet  M4OxPWZ2dmO2aX;uJGF{e2G7 NGH0UFIyyqEQvH2= NIrXb3U2KG2rbh?= M{\FS4lvcGmkaYTzJGZk|rOUSVnBMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9v NY\jPIlZOjF6NEi2PVQ>
platelet  NHXqO4lHfW6ldHnvckBCe3OjeR?= M{O0OlAvODVxMT:yMlUh|ryP M4GyUFUhdWmw NFHUW4dqdmirYnn0d{B1cGVic3nncoFtcW6pIH3lZ4hidmm|bYOg[I94dnO2cnXhcUBw\iCIY98zVmlKSQ>? NYm0ZphQOjF6NEi2PVQ>
DoHH2 M{DJdmFxd3C2b4Ppd{BCe3OjeR?= NX;0[VJJOC9|L{GwJO69VQ>? M1zQb|Q5KGh? M2P1T4lv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NVroNVZ6OjB6N{W0NFg>
Jeko-1  MYXBdI9xfG:|aYOgRZN{[Xl? MYWwM|MwOTBizszN M2fBT|Q5KGh? NUe0dIZ4cW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MXqyNFg4PTRyOB?=
Raji  MX3BdI9xfG:|aYOgRZN{[Xl? NYWzXml3OC9|L{GwJO69VQ>? NY\ZflB3PDhiaB?= MYfpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? NU\zVopFOjB6N{W0NFg>
DHL4 MVLBdI9xfG:|aYOgRZN{[Xl? NFTrVZQxNzFxNDFOwG0> Mn3yPVYhcA>? NVizUVROcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M{[0ZlE5ODB4Nkm2
LY7 NYm2d|JVSXCxcITvd4l{KEG|c3H5 MYmwM|EwPCEQvF2= NY\y[XdCQTZiaB?= NYDNXmJScW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MXKxPFAxPjZ7Nh?=
LY3 NYTTfWNiSXCxcITvd4l{KEG|c3H5 Ml7kNE8yNzRizszN NHPZc5o6PiCq MYTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NHHWUVAyQDByNk[5Oi=>
DHL6 MorPRZBweHSxc3nzJGF{e2G7 MkDjNE8yNzRizszN MX:5OkBp NYPXNpY3cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NV:3dGV1OThyME[2PVY>
LY10 MlTVRZBweHSxc3nzJGF{e2G7 MmDTNE8yNzRizszN NYTBR2RCQTZiaB?= NUnD[FJHcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NXewZ3lSOThyME[2PVY>
DHL10 MULBdI9xfG:|aYOgRZN{[Xl? NYSxUWFrOC9zL{Sg{txO NUDj[WZZQTZiaB?= MYHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NHmybXAyQDByNk[5Oi=>
Wsu-NHL MlzDRZBweHSxc3nzJGF{e2G7 NG\WO|MxNzFxNDFOwG0> NVi3ZXFTQTZiaB?= MXPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MX2xPFAxPjZ7Nh?=
LY18 NGrZNpRCeG:ydH;zbZMhSXO|YYm= MoHSNE8yNzRizszN M{j3WFk3KGh? NGfmSHNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NHjMOm8yQDByNk[5Oi=>
LY1 Ml\5RZBweHSxc3nzJGF{e2G7 MYmwM|EwPCEQvF2= NVvvdohyQTZiaB?= MljtbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MUGxPFAxPjZ7Nh?=
DHL8 NVHWUI1mSXCxcITvd4l{KEG|c3H5 MXewM|EwPCEQvF2= NGTHVGU6PiCq NFjpdVZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M2nm[FE5ODB4Nkm2
DHL4 M2T2R2Fxd3C2b4Ppd{BCe3OjeR?= NYC4O3AzPCEQvF2= M1rvTlk3KGh? NVnHSnFpcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? M{j1WlE5ODB4Nkm2
DHL6 MY\BdI9xfG:|aYOgRZN{[Xl? M2jUW|Qh|ryP NUn2VoJlQTZiaB?= MmPibY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MYGxPFAxPjZ7Nh?=
LY3 MUnBdI9xfG:|aYOgRZN{[Xl? M1rTRlQh|ryP NYrLNWt3QTZiaB?= Mlj6bY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MWGxPFAxPjZ7Nh?=
LY7 NXjzOItKSXCxcITvd4l{KEG|c3H5 M2LzPFQh|ryP M1LYcVk3KGh? MlPVbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MYKxPFAxPjZ7Nh?=
DHL4 NEDGd3lHfW6ldHnvckBCe3OjeR?= M4PLW|Qh|ryP NXPGd5V7OTZiaB?= M3HtdolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NGjncYwyQDByNk[5Oi=>
LY7 NUj3PWtXTnWwY4Tpc44hSXO|YYm= NIO2cpk1KM7:TR?= Mm\sNVYhcA>? M3zre4lvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M3S2clE5ODB4Nkm2
LY3 MULGeY5kfGmxbjDBd5NigQ>? M3fTVFQh|ryP NVzldoVzOTZiaB?= M{G2eIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NInxRVkyQDByNk[5Oi=>
DHL6 MUPGeY5kfGmxbjDBd5NigQ>? NXXq[4lvPCEQvF2= NYLoc3JmOTZiaB?= MVLpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NXHXdYREOThyME[2PVY>
LY10 M372ZWZ2dmO2aX;uJGF{e2G7 NInQcGE1KM7:TR?= MUSxOkBp M1;4ZolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MXyxPFAxPjZ7Nh?=
Wsu-NHL MoHHSpVv[3Srb36gRZN{[Xl? NH72XpA1KM7:TR?= MVSxOkBp NFXwb3lqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MVKxPFAxPjZ7Nh?=
LY18 Mn3DSpVv[3Srb36gRZN{[Xl? M{fyfFQh|ryP MVSxOkBp M2mySYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NHLpbG8yQDByNk[5Oi=>

... 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
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 CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C.C1=CC=C(C=C1)S(=O)(=O)O

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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.

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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