R406

For research use only.

Catalog No.S2194

49 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 286 In stock
USD 120 In stock
USD 170 In stock
USD 270 In stock
USD 870 In stock
USD 1990 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's R406 has been cited by 49 publications

Purity & Quality Control

Choose Selective Syk Inhibitors

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 M2D6dWZ2dmO2aX;uJGF{e2G7 NX;FWYFXOSEQvF2= MojkN:KhcA>? NIXDbXlz\WS3Y3XzJI1q\3KjdHnvcuKh MVGyOlI2OTd4MR?=
U266 M1jqWGZ2dmO2aX;uJGF{e2G7 M3vjS|Eh|ryP NUfSTYtGO8LiaB?= M1PrNpJm\HWlZYOgcYloemG2aX;uxsA> MoH5NlYzPTF5NkG=
Jeko-1 NUnQNVVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe0PEBp MXTJR|UxRTVwME[4NlYh|ryP MWCyOVg{PTd3NR?=
Mino MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTkOFghcA>? M2fpc2lEPTB;NT63NFg2PCEQvF2= MX:yOVg{PTd3NR?=
Jeko-1 MlPiRZBweHSxc3nzJGF{e2G7 M3z1T|XDqM7:TR?= NUXUNox[OjRiaB?= MYHpcoR2[2W|IEK1MlHDqMLzwrCzMlLDqCViYYDvdJRwe2m| MmnJNlU5OzV5NUW=
primary MCL MluzRZBweHSxc3nzJGF{e2G7 NUHWbZV{OiEEtV2= NFrjdpQzPCCq NIXFdIxqdmO{ZXHz[ZMhe2mpbnnmbYNidnSueTDhdI9xfG:|aYRCpC=> MXiyOVM5QDN5Mx?=
PBMCs MnmxR4VtdCCYaXHibYxqfHliQYPzZZk> NV3zWY9UOC13MDFOwG0> MV2yOEBp NEH2eWVFVVOR NYrIN4pWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NFLyU5IzPTF{N{i2Ni=>
PBMCs MULGeY5kfGmxbjDBd5NigQ>? MYO1JO69VQ>? M2nuU|EhcA>? MY\EUXNQ MWLk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u MnXDNlUyOjd6NkK=
CFSE-CD4+ T  MoPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3j4[VAvODZ{NT2xJO69VQ>? NFv6S4s1KGR? NY\4RXFz[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= M{TSPFI1Pjd7OUiy
CFSE-CD11b+ NI\BUXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi0PW1XOC5yNkK1MVEh|ryP NYLhcZE1QCCm NUPISYVZ[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= NHXIPFgzPDZ5OUm4Ni=>
HMECs M4LhVmZ2dmO2aX;uJGF{e2G7 MXywMVExKM7:TR?= MVuyNEBucW5? NHrVNYFqdmirYnn0d{BXTUeILYP0bY12dGG2ZXSgdoVt\WG|ZTDv[kBPVw>? M3z1eFI1OzJ7NUS0
AB5 NV;HbJBiSXCxcITvd4l{KEG|c3H5 NG[xcnAxNTJwNTFOwG0> NGLnZZE1QCCq M332Z2ROW09? NIjiT3dqdmS3Y3XzJIFxd3C2b4Ppdy=> M{TnV|I{Ozl6OUGx
JB7 MXzBdI9xfG:|aYOgRZN{[Xl? NIXTfm8xNTJwNTFOwG0> M3;0clQ5KGh? MXvEUXNQ NF3YPHZqdmS3Y3XzJIFxd3C2b4Ppdy=> NVPpTmlQOjN|OUi5NVE>
AB5 M2TETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHhTmkxNTJwNTFOwG0> NGjLfHk1QCCq NILk[3BFVVOR MV3pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MmryNlM{QTh7MUG=
JB7 NF7sSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOwMVIvPSEQvF2= NX;hTmdlPDhiaB?= MUHEUXNQ NVjrfFlvcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NVrzVIl2OjN|OUi5NVE>
RL MnfYSpVv[3Srb36gRZN{[Xl? MXqyMlUwPSEQvF2= MVOyOE81QCCq MXnEUXNQ NYfISpFjcW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= MlvsNlE6OjZ7NkW=
RL MkO5SpVv[3Srb36gRZN{[Xl? MkjvNU8zNjVizszN NYLaPHU3OjRiaB?= NFfQdWRFVVOR MlTTdoVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? NFGxcXAzOTl{Nkm2OS=>
platelet  NXfZOphmTnWwY4Tpc44hSXO|YYm= NVjpSGEzOcLizszt MkftOUBucW5? MWPpcohq[mm2czDGZ:6{WkmLQT3t[YRq[XSnZDDwcIF1\WyndDDh[4dz\WejdHnvci=> MnryNlE5PDh4OUS=
platelet  M2nZWWZ2dmO2aX;uJGF{e2G7 NEnjPIIxNjB3L{GvNk42KM7:TR?= M{HCVFUhdWmw M1nVc4lvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC M{i3e|IyQDR6Nkm0
DoHH2 M321fGFxd3C2b4Ppd{BCe3OjeR?= NWHldJBPOC9|L{GwJO69VQ>? NYLId|UxPDhiaB?= NWHGb2pKcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MUOyNFg4PTRyOB?=
Jeko-1  NIjq[GNCeG:ydH;zbZMhSXO|YYm= MnPnNE8{NzFyIN88US=> NX75U4Z6PDhiaB?= NV3M[5RVcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NFvQTmIzODh5NUSwPC=>
Raji  NEGyR4tCeG:ydH;zbZMhSXO|YYm= MYOwM|MwOTBizszN NIPURYc1QCCq MlnPbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? MofQNlA5PzV2MEi=
DHL4 MonGRZBweHSxc3nzJGF{e2G7 M4qxR|AwOS92IN88US=> MmHqPVYhcA>? MWHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MUixPFAxPjZ7Nh?=
LY7 NFni[29CeG:ydH;zbZMhSXO|YYm= NXHIRWVMOC9zL{Sg{txO NWi4ZlJbQTZiaB?= Mm\GbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHvHZ4syQDByNk[5Oi=>
LY3 M4i2fWFxd3C2b4Ppd{BCe3OjeR?= NFPRPYwxNzFxNDFOwG0> M1PjWlk3KGh? MoDvbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MVKxPFAxPjZ7Nh?=
DHL6 NUn4dVdQSXCxcITvd4l{KEG|c3H5 MWOwM|EwPCEQvF2= MUC5OkBp M4T0NIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MVexPFAxPjZ7Nh?=
LY10 Mk\hRZBweHSxc3nzJGF{e2G7 NYPqPJBvOC9zL{Sg{txO M2f1PFk3KGh? MmfhbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M2DCfVE5ODB4Nkm2
DHL10 NF3JO|dCeG:ydH;zbZMhSXO|YYm= NYGzc2ZEOC9zL{Sg{txO Mon0PVYhcA>? NYnR[GNHcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M4TpU|E5ODB4Nkm2
Wsu-NHL MYHBdI9xfG:|aYOgRZN{[Xl? MonPNE8yNzRizszN NI\VV3k6PiCq NYTmSndwcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MXmxPFAxPjZ7Nh?=
LY18 MYXBdI9xfG:|aYOgRZN{[Xl? MoruNE8yNzRizszN NHn0e3Q6PiCq NGfudlRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MkTnNVgxODZ4OU[=
LY1 NV3nTFFvSXCxcITvd4l{KEG|c3H5 MXiwM|EwPCEQvF2= NFHhWIo6PiCq MXnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MVqxPFAxPjZ7Nh?=
DHL8 MkjLRZBweHSxc3nzJGF{e2G7 MY[wM|EwPCEQvF2= M1rXSVk3KGh? NXXHc5l3cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M3LGUFE5ODB4Nkm2
DHL4 MWjBdI9xfG:|aYOgRZN{[Xl? MlTWOEDPxE1? NVixc|doQTZiaB?= NXW1UpdvcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? NHPrTJQyQDByNk[5Oi=>
DHL6 MlLNRZBweHSxc3nzJGF{e2G7 MXu0JO69VQ>? MVW5OkBp NXz6boxRcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? M3zmN|E5ODB4Nkm2
LY3 NGDOdplCeG:ydH;zbZMhSXO|YYm= M{TCclQh|ryP Mm[2PVYhcA>? NELHboJqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NGrlO5gyQDByNk[5Oi=>
LY7 NE\JcphCeG:ydH;zbZMhSXO|YYm= NYPaWmVyPCEQvF2= NVnxUlZ[QTZiaB?= NFHsZ|RqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 Mne1NVgxODZ4OU[=
DHL4 NWTaUWRjTnWwY4Tpc44hSXO|YYm= MUK0JO69VQ>? MUGxOkBp MoPkbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NWP4NHFVOThyME[2PVY>
LY7 M165T2Z2dmO2aX;uJGF{e2G7 MXm0JO69VQ>? MVexOkBp NHm2XWFqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MnjkNVgxODZ4OU[=
LY3 NXToZ4RtTnWwY4Tpc44hSXO|YYm= NUjkdGlYPCEQvF2= MWOxOkBp M4nFZYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NGLUNYQyQDByNk[5Oi=>
DHL6 NEDqfJJHfW6ldHnvckBCe3OjeR?= M2PQelQh|ryP M{SwelE3KGh? NFzvNVdqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NETWRVUyQDByNk[5Oi=>
LY10 M374eGZ2dmO2aX;uJGF{e2G7 MXu0JO69VQ>? NHzBOFYyPiCq NWnnR3VCcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MWOxPFAxPjZ7Nh?=
Wsu-NHL M4HuZmZ2dmO2aX;uJGF{e2G7 NWXDSG9{PCEQvF2= NFW4RZUyPiCq NYPLOmZncW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MY[xPFAxPjZ7Nh?=
LY18 NY\I[YdxTnWwY4Tpc44hSXO|YYm= NVn4cm53PCEQvF2= Mn7CNVYhcA>? M{P6ZYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u M1z4elE5ODB4Nkm2

... 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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

Syk Inhibitors with Unique Features

Related Syk Products

Tags: buy R406 | R406 supplier | purchase R406 | R406 cost | R406 manufacturer | order R406 | R406 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID