R406

For research use only. Not for use in humans.

Catalog No.S2194

37 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 37 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 MVnGeY5kfGmxbjDBd5NigQ>? NUPoRZVFOSEQvF2= M3TFNlPDqGh? MnPxdoVlfWOnczDtbYdz[XSrb39CpC=> M{jhWVI3OjVzN{[x
U266 MUjGeY5kfGmxbjDBd5NigQ>? MlX4NUDPxE1? MnfnN:KhcA>? NXTH[GYyemWmdXPld{BucWe{YYTpc47DqA>? NFTLOngzPjJ3MUe2NS=>
Jeko-1 NUjKWpNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[0PEBp Ml:3TWM2OD13LkC2PFI3KM7:TR?= NG\xWVUzPTh|NUe1OS=>
Mino M2TTZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy0PEBp NHm3PJNKSzVyPUWuO|A5PTRizszN MoHNNlU5OzV5NUW=
Jeko-1 NVTWRWhjSXCxcITvd4l{KEG|c3H5 NH32V5Q2yqEQvF2= NIjoUIMzPCCq M1zBdIlv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= M1TlS|I2QDN3N{W1
primary MCL NF7Ge3lCeG:ydH;zbZMhSXO|YYm= NFSwfm8zKML3TR?= MlrqNlQhcA>? MnL4bY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= MmroNlU{QDh|N{O=
PBMCs M2PZXmNmdGxiVnnhZoltcXS7IFHzd4F6 MnXNNE02OCEQvF2= MYOyOEBp M1vaNWROW09? M{S4XolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NXixV3pzOjVzMke4OlI>
PBMCs NF;QXnBHfW6ldHnvckBCe3OjeR?= NX:3R3JrPSEQvF2= Mm\XNUBp NY\RdZRnTE2VTx?= NGSwVXll\WO{ZXHz[ZMhfGinIHPlcIwhdWmpcnH0bY9v MUmyOVEzPzh4Mh?=
CFSE-CD4+ T  MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvENG9ZOC5yNkK1MVEh|ryP MonVOEBl NHXTenVjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= NVjYNJhJOjR4N{m5PFI>
CFSE-CD11b+ NHvCUJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjUNE4xPjJ3LUGg{txO MYm4JIQ> NXezS5Vq[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= MYCyOFY4QTl6Mh?=
HMECs MlrGSpVv[3Srb36gRZN{[Xl? M2XoZVAuOTBizszN MlXpNlAhdWmw MkPpbY5pcWKrdIOgWmVITi2|dHnteYxifGWmIILlcIVie2Vib3[gUm8> MmL5NlQ{Ojl3NES=
AB5 M17uTWFxd3C2b4Ppd{BCe3OjeR?= NGq1b3QxNTJwNTFOwG0> M4foTVQ5KGh? MkHLSG1UVw>? MoKxbY5lfWOnczDhdI9xfG:|aYO= Ml64NlM{QTh7MUG=
JB7 NXvGUmZRSXCxcITvd4l{KEG|c3H5 M3fNflAuOi53IN88US=> NH3Mclg1QCCq MYHEUXNQ NYXGeZdYcW6mdXPld{BieG:ydH;zbZM> M3\UU|I{Ozl6OUGx
AB5 NWn2O5hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHZTGRtOC1{LkWg{txO M1[yfFQ5KGh? MX7EUXNQ MUXpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MU[yN|M6QDlzMR?=
JB7 NHTWVodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqwMVIvPSEQvF2= MUC0PEBp MYnEUXNQ NH;lZ5lqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M3Gzc|I{Ozl6OUGx
RL MX\GeY5kfGmxbjDBd5NigQ>? MWOyMlUwPSEQvF2= NGjKWZUzPC92ODDo M1[0PWROW09? NFr1e2hqdmS3Y3XzJIEheG:2ZX70JIRm[3KnYYPlJIlvKE2PUD25JI1TVkFiZYjwdoV{e2mxbh?= M1TEN|IyQTJ4OU[1
RL NVezfXU5TnWwY4Tpc44hSXO|YYm= NFPxNJAyNzJwNTFOwG0> NF;KN4szPCCq MmXUSG1UVw>? M{TCVJJm\HWlZYOgeIhmKGGldHn2ZZRqd25ib3[gRYt1KGGwZDDwO|BUPkt? M4j1cVIyQTJ4OU[1
platelet  M4izdWZ2dmO2aX;uJGF{e2G7 NFvkV4oyyqEQvH2= NFnmcVU2KG2rbh?= M2DhWolvcGmkaYTzJGZk|rOUSVnBMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9v NYDKbm46OjF6NEi2PVQ>
platelet  NWjTRYdWTnWwY4Tpc44hSXO|YYm= M2e4XlAvODVxMT:yMlUh|ryP MV21JI1qdg>? M3v3WolvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC M4foU|IyQDR6Nkm0
DoHH2 NWnsVlFwSXCxcITvd4l{KEG|c3H5 MX[wM|MwOTBizszN NIT5SZo1QCCq MX3pcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? MmCyNlA5PzV2MEi=
Jeko-1  MY\BdI9xfG:|aYOgRZN{[Xl? NIX5bGUxNzNxMUCg{txO NGfmbFg1QCCq M{L4cYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 M{Hwd|IxQDd3NEC4
Raji  MlH1RZBweHSxc3nzJGF{e2G7 NX7vPIdMOC9|L{GwJO69VQ>? NVfTUHg6PDhiaB?= NGLVb45qdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NGDpeoYzODh5NUSwPC=>
DHL4 NHu2cldCeG:ydH;zbZMhSXO|YYm= NWjteod4OC9zL{Sg{txO NIjmZYw6PiCq NIi0SodqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MXOxPFAxPjZ7Nh?=
LY7 NHvlPWtCeG:ydH;zbZMhSXO|YYm= NIjnUFYxNzFxNDFOwG0> NX3kco1QQTZiaB?= MkT3bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHf6PZkyQDByNk[5Oi=>
LY3 NVLZRWVsSXCxcITvd4l{KEG|c3H5 M{TQOlAwOS92IN88US=> MWe5OkBp M2nSZYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NFvZXJgyQDByNk[5Oi=>
DHL6 M13PeGFxd3C2b4Ppd{BCe3OjeR?= M1q3SFAwOS92IN88US=> NU\NTFJKQTZiaB?= M3rSZolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NX70d5F5OThyME[2PVY>
LY10 MofzRZBweHSxc3nzJGF{e2G7 NE\4UW0xNzFxNDFOwG0> MX65OkBp NEPHOnZqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NYPMe|lROThyME[2PVY>
DHL10 NYKwW5R2SXCxcITvd4l{KEG|c3H5 NY[3Z|Q4OC9zL{Sg{txO MmnhPVYhcA>? M32weIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M4PEbFE5ODB4Nkm2
Wsu-NHL NUXPeoNiSXCxcITvd4l{KEG|c3H5 NIX0V|MxNzFxNDFOwG0> MmfnPVYhcA>? NX[3clZlcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NUPwZ29POThyME[2PVY>
LY18 NFLD[HFCeG:ydH;zbZMhSXO|YYm= NU\Penl1OC9zL{Sg{txO NULHSIdNQTZiaB?= MYDpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MkXsNVgxODZ4OU[=
LY1 Mo\aRZBweHSxc3nzJGF{e2G7 M1i3ZlAwOS92IN88US=> Mnf1PVYhcA>? M3\UUolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NX;xNmw2OThyME[2PVY>
DHL8 M1XoN2Fxd3C2b4Ppd{BCe3OjeR?= NVviTXpkOC9zL{Sg{txO NX\KeVJkQTZiaB?= MlTDbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MX6xPFAxPjZ7Nh?=
DHL4 MlTpRZBweHSxc3nzJGF{e2G7 MUS0JO69VQ>? NEP3S4I6PiCq MXrpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NHmxWGUyQDByNk[5Oi=>
DHL6 M4PVOWFxd3C2b4Ppd{BCe3OjeR?= MkjiOEDPxE1? M3u5bFk3KGh? NWLocnJOcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? M4Pv[lE5ODB4Nkm2
LY3 MV7BdI9xfG:|aYOgRZN{[Xl? M1m4T|Qh|ryP M3zDd|k3KGh? M{XqTolv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MmHJNVgxODZ4OU[=
LY7 MkT0RZBweHSxc3nzJGF{e2G7 MmDjOEDPxE1? M2L2dlk3KGh? Mo\TbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> NFGxW2gyQDByNk[5Oi=>
DHL4 M3XXUWZ2dmO2aX;uJGF{e2G7 M{jne|Qh|ryP NVPxSHR1OTZiaB?= NXvlb|hzcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NHnkU4kyQDByNk[5Oi=>
LY7 NV3PSoNnTnWwY4Tpc44hSXO|YYm= NIfnTnU1KM7:TR?= M{jlPVE3KGh? M{HQfYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NIq0dXIyQDByNk[5Oi=>
LY3 M13UWGZ2dmO2aX;uJGF{e2G7 M{j0NFQh|ryP MVyxOkBp M{\HNolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M{nUOFE5ODB4Nkm2
DHL6 MoG0SpVv[3Srb36gRZN{[Xl? NWj4XXdzPCEQvF2= NIDNeJcyPiCq NEK5V45qdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MUmxPFAxPjZ7Nh?=
LY10 MWHGeY5kfGmxbjDBd5NigQ>? M1XFelQh|ryP MYixOkBp MoLFbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= M3fGU|E5ODB4Nkm2
Wsu-NHL MXjGeY5kfGmxbjDBd5NigQ>? MljGOEDPxE1? NIX5cIUyPiCq Mn2wbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= Ml\DNVgxODZ4OU[=
LY18 NYD3cI5OTnWwY4Tpc44hSXO|YYm= Mn7kOEDPxE1? NED0Z4syPiCq MoTFbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MVexPFAxPjZ7Nh?=

... 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.
  • 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(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.

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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