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R406

For research use only.

Catalog No.S2194

55 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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10mM (1mL in DMSO) USD 286 In stock
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Selleck's R406 has been cited by 55 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 Ml2wSpVv[3Srb36gRZN{[Xl? NIDT[ZUyKM7:TR?= MWSzxsBp MlGwdoVlfWOnczDtbYdz[XSrb39CpC=> NXLkSXpvOjZ{NUG3OlE>
U266 M2HDcWZ2dmO2aX;uJGF{e2G7 MVOxJO69VQ>? NXHTTW9IO8LiaB?= NHf6dHFz\WS3Y3XzJI1q\3KjdHnvcuKh NFrFXlczPjJ3MUe2NS=>
Jeko-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzX[ms1QCCq M2TQPWlEPTB;NT6wOlgzPiEQvF2= NVz2NopSOjV6M{W3OVU>
Mino Ml6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:0PEBp NUnNeIJyUUN3ME21MlcxQDV2IN88US=> M2DTeVI2QDN3N{W1
Jeko-1 MnLqRZBweHSxc3nzJGF{e2G7 MUK1xsDPxE1? MmPQNlQhcA>? NVP2eItYcW6mdXPld{AzPS5zwrFCteKhOy5{wrClJIFxd3C2b4Ppdy=> MYeyOVg{PTd3NR?=
primary MCL NXzwV29ESXCxcITvd4l{KEG|c3H5 M2HKRlIhyrWP MonPNlQhcA>? MV3pcoNz\WG|ZYOgd4lodmmoaXPhcpRtgSCjcH;weI9{cXQEoB?= MUiyOVM5QDN5Mx?=
PBMCs MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnTUNE02OCEQvF2= NU\3NWszOjRiaB?= NEPDPVFFVVOR MVfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M2jieVI2OTJ5OE[y
PBMCs MVzGeY5kfGmxbjDBd5NigQ>? MWm1JO69VQ>? M1ziWVEhcA>? NGf0XnZFVVOR MYTk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u M{L1UlI2OTJ5OE[y
CFSE-CD4+ T  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPlNE4xPjJ3LUGg{txO NYjz[GJ1PCCm M3HTOoJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| NG\PSXozPDZ5OUm4Ni=>
CFSE-CD11b+ NYjMU5F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMlA3OjVvMTFOwG0> M4TIblgh\A>? NF3L[oNjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= NWHDTodLOjR4N{m5PFI>
HMECs Mlq3SpVv[3Srb36gRZN{[Xl? NYXEUFVKOC1zMDFOwG0> M1nRUFIxKG2rbh?= NXK0TmlNcW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? MoP5NlQ{Ojl3NES=
AB5 NGPyflhCeG:ydH;zbZMhSXO|YYm= NWOwR3hoOC1{LkWg{txO MnLhOFghcA>? NIHRPW5FVVOR NEHp[WVqdmS3Y3XzJIFxd3C2b4Ppdy=> NUO5NJQ6OjN|OUi5NVE>
JB7 MofPRZBweHSxc3nzJGF{e2G7 M3f5PVAuOi53IN88US=> NHK5XY01QCCq NFmzd29FVVOR MVfpcoR2[2W|IHHwc5B1d3Orcx?= NUDHdXZrOjN|OUi5NVE>
AB5 NYPtS|luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorTNE0zNjVizszN NWXUSGpNPDhiaB?= MmrUSG1UVw>? NXrRVpZYcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M{HBNlI{Ozl6OUGx
JB7 NEPt[5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrKNE0zNjVizszN NX7XO21CPDhiaB?= NW\ZVVhwTE2VTx?= M373bIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHz2[mIzOzN7OEmxNS=>
RL MljKSpVv[3Srb36gRZN{[Xl? M{C2PVIvPS93IN88US=> MYKyOE81QCCq M4H3XGROW09? MlTKbY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? MmjSNlE6OjZ7NkW=
RL MVnGeY5kfGmxbjDBd5NigQ>? MUWxM|IvPSEQvF2= Mn7TNlQhcA>? NX3vWJJMTE2VTx?= NHrEO4Zz\WS3Y3XzJJRp\SCjY4TpeoF1cW:wIH;mJGFsfCCjbnSgdFcxWz[N MWmyNVkzPjl4NR?=
platelet  NUDMU5Y6TnWwY4Tpc44hSXO|YYm= MYixxsDPxG1? NG\zZVQ2KG2rbh?= MV3pcohq[mm2czDGZ:6{WkmLQT3t[YRq[XSnZDDwcIF1\WyndDDh[4dz\WejdHnvci=> NGL6NVAzOTh2OE[5OC=>
platelet  NFXoRoNHfW6ldHnvckBCe3OjeR?= MWKwMlA2NzFxMj61JO69VQ>? NXfYZpd2PSCvaX6= M{X0dYlvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC MljONlE5PDh4OUS=
DoHH2 MkDxRZBweHSxc3nzJGF{e2G7 NIK0cpQxNzNxMUCg{txO M330fVQ5KGh? MWrpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? M3TSclIxQDd3NEC4
Jeko-1  NWnSVVRUSXCxcITvd4l{KEG|c3H5 NFex[owxNzNxMUCg{txO M1izcFQ5KGh? MXzpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? Mk\WNlA5PzV2MEi=
Raji  MUXBdI9xfG:|aYOgRZN{[Xl? MWCwM|MwOTBizszN NX3nTnNRPDhiaB?= NX\sVXJqcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MmP6NlA5PzV2MEi=
DHL4 M2ToW2Fxd3C2b4Ppd{BCe3OjeR?= MVSwM|EwPCEQvF2= NF3rbXY6PiCq MlntbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M3nTSlE5ODB4Nkm2
LY7 MVrBdI9xfG:|aYOgRZN{[Xl? M{D4fVAwOS92IN88US=> NYLR[YZJQTZiaB?= Ml7obY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MYCxPFAxPjZ7Nh?=
LY3 MoPPRZBweHSxc3nzJGF{e2G7 MVywM|EwPCEQvF2= Mn75PVYhcA>? Mni2bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NUL0e3A4OThyME[2PVY>
DHL6 NGDBT2hCeG:ydH;zbZMhSXO|YYm= M{DMblAwOS92IN88US=> MYG5OkBp NWm5bpF4cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYTmco1EOThyME[2PVY>
LY10 MljjRZBweHSxc3nzJGF{e2G7 NHrlOHAxNzFxNDFOwG0> NYfYNnU4QTZiaB?= M4G1RYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NGXLTlUyQDByNk[5Oi=>
DHL10 MX\BdI9xfG:|aYOgRZN{[Xl? NXP6TlNiOC9zL{Sg{txO M4\rR|k3KGh? M1TJUIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M4DmbFE5ODB4Nkm2
Wsu-NHL MoPmRZBweHSxc3nzJGF{e2G7 NIfVN4IxNzFxNDFOwG0> M2Prelk3KGh? MnfWbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NWLPR2NLOThyME[2PVY>
LY18 MVHBdI9xfG:|aYOgRZN{[Xl? NG[yS|ExNzFxNDFOwG0> NWLNfZZJQTZiaB?= MVLpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M4TEOlE5ODB4Nkm2
LY1 MoLuRZBweHSxc3nzJGF{e2G7 MnrlNE8yNzRizszN Mke3PVYhcA>? NHzpWZlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NX3BU3pSOThyME[2PVY>
DHL8 NFv0ZZhCeG:ydH;zbZMhSXO|YYm= MXmwM|EwPCEQvF2= M2XYelk3KGh? NYDXZ|R4cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> Mn3PNVgxODZ4OU[=
DHL4 MoDWRZBweHSxc3nzJGF{e2G7 MYi0JO69VQ>? MVq5OkBp MoPVbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MVqxPFAxPjZ7Nh?=
DHL6 NXnGUYx4SXCxcITvd4l{KEG|c3H5 M1\3UVQh|ryP MXu5OkBp MnHNbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> NIq3NJMyQDByNk[5Oi=>
LY3 MnvxRZBweHSxc3nzJGF{e2G7 NICwXno1KM7:TR?= MnvlPVYhcA>? NIm2XVlqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MoH3NVgxODZ4OU[=
LY7 M4nLbGFxd3C2b4Ppd{BCe3OjeR?= M1jCR|Qh|ryP NYizdIdGQTZiaB?= MlntbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> M{m1Z|E5ODB4Nkm2
DHL4 NGnFeYVHfW6ldHnvckBCe3OjeR?= NX;jO3hCPCEQvF2= NETxTHgyPiCq MUfpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NYf0R|hqOThyME[2PVY>
LY7 NYHCVnZxTnWwY4Tpc44hSXO|YYm= M4TlPFQh|ryP MW[xOkBp M4DHOIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NWTiUIR2OThyME[2PVY>
LY3 M3PSWWZ2dmO2aX;uJGF{e2G7 NV;t[oFjPCEQvF2= M332XVE3KGh? M2DVSolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NEfMdoQyQDByNk[5Oi=>
DHL6 MlfFSpVv[3Srb36gRZN{[Xl? M3nCU|Qh|ryP NGfpT2wyPiCq M33yZ4lvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MofjNVgxODZ4OU[=
LY10 NYLCS|dWTnWwY4Tpc44hSXO|YYm= MmP4OEDPxE1? NYXG[Vk4OTZiaB?= NW[5PZNwcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MnT1NVgxODZ4OU[=
Wsu-NHL NVvUeolITnWwY4Tpc44hSXO|YYm= M4TCRlQh|ryP M3:yUFE3KGh? NX7KSFZFcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> MlKxNVgxODZ4OU[=
LY18 MYfGeY5kfGmxbjDBd5NigQ>? M1u3WlQh|ryP NYPab|RJOTZiaB?= NVrP[4tRcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> Mn\WNVgxODZ4OU[=

... 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 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.

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