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.

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In DMSO USD 286 In stock
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Cited by 34 Publications

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 M4m1RmZ2dmO2aX;uJGF{e2G7 MUixJO69VQ>? NF:3R5A{yqCq NXzR[Il[emWmdXPld{BucWe{YYTpc47DqA>? NGPySFczPjJ3MUe2NS=>
U266 NYP6clk4TnWwY4Tpc44hSXO|YYm= NWPmZoZzOSEQvF2= M2HPV|PDqGh? NYL3c5ZEemWmdXPld{BucWe{YYTpc47DqA>? M{DPdFI3OjVzN{[x
Jeko-1 NGXFVmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fScVQ5KGh? NFfhdGlKSzVyPUWuNFY5OjZizszN NEW2U|gzPTh|NUe1OS=>
Mino M2\Pb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrZ[4I1QCCq MUXJR|UxRTVwN{C4OVQh|ryP MVyyOVg{PTd3NR?=
Jeko-1 NWHnOY1OSXCxcITvd4l{KEG|c3H5 MV61xsDPxE1? MXeyOEBp NIXTR2VqdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz NYLFdYJ{OjV6M{W3OVU>
primary MCL MVPBdI9xfG:|aYOgRZN{[Xl? NUjhfm5zOiEEtV2= NXLMUotROjRiaB?= MmXxbY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= NEHDXYszPTN6OEO3Ny=>
PBMCs M4HsPWNmdGxiVnnhZoltcXS7IFHzd4F6 MkPlNE02OCEQvF2= M3n1d|I1KGh? NGXhWnJFVVOR NYXyd3dycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NIPQUm0zPTF{N{i2Ni=>
PBMCs NHPPTmtHfW6ldHnvckBCe3OjeR?= NGDkU|E2KM7:TR?= NVHoTHRrOSCq NGPGfI9FVVOR NVPQVpVi\GWlcnXhd4V{KHSqZTDj[YxtKG2rZ4LheIlwdg>? NWLLTXZ4OjVzMke4OlI>
CFSE-CD4+ T  Mnn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jxWFAvODZ{NT2xJO69VQ>? MUK0JIQ> MUTicI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? M3fjO|I1Pjd7OUiy
CFSE-CD11b+ M3TCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzlUIJQOC5yNkK1MVEh|ryP MV24JIQ> NE\ZeHRjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= NFfJWZczPDZ5OUm4Ni=>
HMECs M{nn[2Z2dmO2aX;uJGF{e2G7 MXmwMVExKM7:TR?= NX[4cpRDOjBibXnu MX\pcohq[mm2czDWSWdHNXO2aX31cIF1\WRicnXs[YF{\SCxZjDOUy=> M3O5V|I1OzJ7NUS0
AB5 M3HqemFxd3C2b4Ppd{BCe3OjeR?= MmXkNE0zNjVizszN M2\yRVQ5KGh? M2PNTGROW09? Mm\VbY5lfWOnczDhdI9xfG:|aYO= NVi1VHVFOjN|OUi5NVE>
JB7 MkeyRZBweHSxc3nzJGF{e2G7 NHjDS4ExNTJwNTFOwG0> MluxOFghcA>? MoT5SG1UVw>? NFvJVmxqdmS3Y3XzJIFxd3C2b4Ppdy=> MkX2NlM{QTh7MUG=
AB5 MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPXNE0zNjVizszN MV[0PEBp MkjWSG1UVw>? MkW3bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NFnib2ozOzN7OEmxNS=>
JB7 NFTEPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOwMVIvPSEQvF2= MX:0PEBp Ml34SG1UVw>? MWjpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M3Hw[|I{Ozl6OUGx
RL M3O0NGZ2dmO2aX;uJGF{e2G7 NGn3XogzNjVxNTFOwG0> M3T5VFI1NzR6IHi= NGPqZoNFVVOR NXjZSZZDcW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= NYLGWHZNOjF7Mk[5OlU>
RL Mnf3SpVv[3Srb36gRZN{[Xl? MYKxM|IvPSEQvF2= M3X4VVI1KGh? NET1NpNFVVOR M37afZJm\HWlZYOgeIhmKGGldHn2ZZRqd25ib3[gRYt1KGGwZDDwO|BUPkt? MkmxNlE6OjZ7NkW=
platelet  M4XsVGZ2dmO2aX;uJGF{e2G7 NE\WNYgyyqEQvH2= MX21JI1qdg>? NXLycJY4cW6qaXLpeJMhTmQQs2LJTWEudWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25? MoD0NlE5PDh4OUS=
platelet  MmriSpVv[3Srb36gRZN{[Xl? NXLqXFJQOC5yNT:xM|IvPSEQvF2= NFnVcI82KG2rbh?= M1y5UYlvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC MYCyNVg1QDZ7NB?=
DoHH2 M4HUO2Fxd3C2b4Ppd{BCe3OjeR?= NH\nXYgxNzNxMUCg{txO NG\3[ms1QCCq M2P2VYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 MYSyNFg4PTRyOB?=
Jeko-1  MV\BdI9xfG:|aYOgRZN{[Xl? Mo\CNE8{NzFyIN88US=> M3jBbVQ5KGh? MkmybY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? NYrpToJEOjB6N{W0NFg>
Raji  MYTBdI9xfG:|aYOgRZN{[Xl? NVj0PI15OC9|L{GwJO69VQ>? NHPi[3U1QCCq MkXhbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? MmrWNlA5PzV2MEi=
DHL4 NHnKdodCeG:ydH;zbZMhSXO|YYm= NVfm[4hNOC9zL{Sg{txO NHj0VIk6PiCq MYrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NGPFR4kyQDByNk[5Oi=>
LY7 NUjubZJxSXCxcITvd4l{KEG|c3H5 MmPPNE8yNzRizszN NInXTnA6PiCq NGjoSXRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4jsWVE5ODB4Nkm2
LY3 M3\semFxd3C2b4Ppd{BCe3OjeR?= NYjyO5BSOC9zL{Sg{txO MkC2PVYhcA>? NETGOJVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4P5eVE5ODB4Nkm2
DHL6 NGHqSnhCeG:ydH;zbZMhSXO|YYm= Mn[1NE8yNzRizszN NVPnbGZKQTZiaB?= NX[4fXF3cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYGxbmlZOThyME[2PVY>
LY10 MnrGRZBweHSxc3nzJGF{e2G7 MYKwM|EwPCEQvF2= M4jNelk3KGh? NIC2dGtqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVy1TZNLOThyME[2PVY>
DHL10 MlOyRZBweHSxc3nzJGF{e2G7 NV3tWWRmOC9zL{Sg{txO NV3zPIw{QTZiaB?= MXPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 Mo\zNVgxODZ4OU[=
Wsu-NHL NFvWW25CeG:ydH;zbZMhSXO|YYm= Mo\zNE8yNzRizszN MUm5OkBp MmS1bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NILw[XMyQDByNk[5Oi=>
LY18 M4HvZ2Fxd3C2b4Ppd{BCe3OjeR?= M17ySFAwOS92IN88US=> NGe2Wok6PiCq MYnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MXyxPFAxPjZ7Nh?=
LY1 Mlf4RZBweHSxc3nzJGF{e2G7 MXewM|EwPCEQvF2= M4PMWFk3KGh? M2T1eIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M{LtUFE5ODB4Nkm2
DHL8 NXjqT|RqSXCxcITvd4l{KEG|c3H5 M4T2WFAwOS92IN88US=> NIjv[VY6PiCq NFjYUpVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Mm\tNVgxODZ4OU[=
DHL4 NHniSXZCeG:ydH;zbZMhSXO|YYm= NV7TSFFnPCEQvF2= NV2zRWFrQTZiaB?= M1j2folv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> M4T1XVE5ODB4Nkm2
DHL6 M1[1cWFxd3C2b4Ppd{BCe3OjeR?= NF;mT3I1KM7:TR?= NYLJUpdUQTZiaB?= MkC4bY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MmfJNVgxODZ4OU[=
LY3 MortRZBweHSxc3nzJGF{e2G7 NXzVNXUxPCEQvF2= NWP5[llsQTZiaB?= M2HQN4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NGDYdlUyQDByNk[5Oi=>
LY7 MkK5RZBweHSxc3nzJGF{e2G7 NEDPSJc1KM7:TR?= NEW3eGU6PiCq M1TjT4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> MmDuNVgxODZ4OU[=
DHL4 M1PR[2Z2dmO2aX;uJGF{e2G7 NWniS41HPCEQvF2= NF3xOmQyPiCq NYHDbphscW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MWSxPFAxPjZ7Nh?=
LY7 NVHoOYNNTnWwY4Tpc44hSXO|YYm= M2DwTlQh|ryP MV2xOkBp NICwUFZqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NXGzSnBXOThyME[2PVY>
LY3 M{myRmZ2dmO2aX;uJGF{e2G7 NHPMS4Q1KM7:TR?= MYOxOkBp NVPobIJFcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> M1j0WlE5ODB4Nkm2
DHL6 NEW5R2RHfW6ldHnvckBCe3OjeR?= MYm0JO69VQ>? MkDINVYhcA>? M4nxSolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NULrOZNoOThyME[2PVY>
LY10 NGrsbY9HfW6ldHnvckBCe3OjeR?= NYXMcolUPCEQvF2= NHLTcm0yPiCq NYmxdHRFcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MlGyNVgxODZ4OU[=
Wsu-NHL MlzoSpVv[3Srb36gRZN{[Xl? MknZOEDPxE1? M3;1dlE3KGh? NVX3TWZrcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MWmxPFAxPjZ7Nh?=
LY18 NUSxVXdRTnWwY4Tpc44hSXO|YYm= NGnZS5Y1KM7:TR?= NWrRWWxvOTZiaB?= NFjJc|FqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NYXqbWh6OThyME[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.
  • 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

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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