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.

Size Price Stock Quantity  
In DMSO USD 286 In stock
USD 120 In stock
USD 170 In stock
USD 270 In stock
USD 870 In stock
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6 Customer Reviews

  • Platelets (3 x 108/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).

    Blood 2014 122(4), 580-9. R406 purchased from Selleck.

    The patient's CLL cells were exposed to dabrafenib, vemurafenib, R406, or DMSO as control at the indicated concentrations, and the resulting Western blot and the RAS-GTP/tRAS ratios are shown. One of 3 independent experiments with similar results is shown.

    J Clin Invest 2014 124(11), 5074-84. R406 purchased from Selleck.

  • (C) Z-138 and JEKO-1 cells were simultaneously  exposed  to sorafenib and R406  at  the  indicated doses, and cell viability was determined at 48 hours by annexin  V/PI  staining.  Bars represent the mean ± SD of 3 independent experiments. CI value is indicated for each combination. (D)  Primary MCL cells from 7 patients were simultaneously exposed to sorafenib and R406 at the indicated doses for 48 hours, and cell viability was determined as above. Bars represent the mean ± SEM of all the samples analyzed. CI value is indicated for each combination.

    Clin Cancer Res 2013 19, 586-597. R406 purchased from Selleck.

    NHEKs were treated with R406 (1 μM) for 1, 3, and 5 days. Then cells were collected for the protein analysis by Western blot.

    J Invest Dermatol, 2016, 136(1):192-201. R406 purchased from Selleck.

  • (M-CSF)-M2 macrophages were exposed to M860-IC (30 µg/ml) for 18 h in the presence of heparin or R406 (0, 1, 3 µM), mAbs against human CD14, CD16, CD32, CD64, or CLI-095 (5 µM). Isotype-matched irrelevant Abs as well as untreated (M-CSF)-M2 cells (M) were included as controls. TNFα in the culture supernatant was quantitated using ELISAs.

    Front Immunol, 2018, 9: 37. R406 purchased from Selleck.

    Neutrophils were pretreated or untreated with the indicated concentrations of R406 for 1 hr. The cells were stimulated with SAA (5 ug/ml) for 4 hr. The cells were harvested and analyzed for NLRP3 mRNA by RT-PCR. Three experiments were performed using different neutrophils and a representative result is shown.

    PLoS One 2014 9(5), e96703. R406 purchased from Selleck.

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. 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 MmH0SpVv[3Srb36gRZN{[Xl? MUixJO69VQ>? MYWzxsBp M4jZWJJm\HWlZYOgcYloemG2aX;uxsA> NWTiSlhROjZ{NUG3OlE>
U266 M1foXWZ2dmO2aX;uJGF{e2G7 MV6xJO69VQ>? MV:zxsBp M{LnUpJm\HWlZYOgcYloemG2aX;uxsA> MUmyOlI2OTd4MR?=
Jeko-1 MlrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlSxOFghcA>? NEnqeJhKSzVyPUWuNFY5OjZizszN MYSyOVg{PTd3NR?=
Mino NHPmV|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3u[pl4PDhiaB?= NEXGPJpKSzVyPUWuO|A5PTRizszN M4joTlI2QDN3N{W1
Jeko-1 M{LBZmFxd3C2b4Ppd{BCe3OjeR?= Ml:1OeKh|ryP NFLWNpEzPCCq M3fuU4lv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= MYKyOVg{PTd3NR?=
primary MCL M1TSbGFxd3C2b4Ppd{BCe3OjeR?= MVWyJOK2VQ>? MkmzNlQhcA>? MkLhbY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= MVeyOVM5QDN5Mx?=
PBMCs NEH3OHNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MonENE02OCEQvF2= M3HWRlI1KGh? NYjSNIJkTE2VTx?= NUXab|FocW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYK0Z5VwOjVzMke4OlI>
PBMCs NX7kU4lMTnWwY4Tpc44hSXO|YYm= NH7WenY2KM7:TR?= NHztbIwyKGh? MUDEUXNQ MmTN[IVkemWjc3XzJJRp\SClZXzsJI1q\3KjdHnvci=> M1i2TFI2OTJ5OE[y
CFSE-CD4+ T  NVP1ZosyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILpcGYxNjB4MkWtNUDPxE1? NIDr[JI1KGR? M3jiNYJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| MWKyOFY4QTl6Mh?=
CFSE-CD11b+ M4DVT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECxO|cxNjB4MkWtNUDPxE1? M2TYN|gh\A>? MYPicI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? MmLkNlQ3Pzl7OEK=
HMECs MkjRSpVv[3Srb36gRZN{[Xl? M1vDcVAuOTBizszN MnXhNlAhdWmw M1r2dolvcGmkaYTzJHZGT0Zvc4TpcZVt[XSnZDDy[Yxm[XOnIH;mJG5Q NILtZokzPDN{OUW0OC=>
AB5 NXjhOng2SXCxcITvd4l{KEG|c3H5 M16yN|AuOi53IN88US=> NFzrVXg1QCCq NUXz[JlQTE2VTx?= Mn7jbY5lfWOnczDhdI9xfG:|aYO= NYPVflg{OjN|OUi5NVE>
JB7 MkO1RZBweHSxc3nzJGF{e2G7 NIK1TGQxNTJwNTFOwG0> M2rlZ|Q5KGh? M4L6OGROW09? NH;mRnZqdmS3Y3XzJIFxd3C2b4Ppdy=> Mnq4NlM{QTh7MUG=
AB5 NXr4ZVlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXWWWwxNTJwNTFOwG0> MUK0PEBp NE\HdZZFVVOR MkTmbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NIOyW5QzOzN7OEmxNS=>
JB7 NGfYU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zJclAuOi53IN88US=> MYG0PEBp NIPUVZhFVVOR M2f5S4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MnntNlM{QTh7MUG=
RL MX;GeY5kfGmxbjDBd5NigQ>? MmjtNk42NzVizszN MWeyOE81QCCq MkDHSG1UVw>? M4rl[Ilv\HWlZYOgZUBxd3SnboSg[IVkemWjc3WgbY4hVU2SLUmgcXJPSSCneIDy[ZN{cW:w M{TRRlIyQTJ4OU[1
RL MWLGeY5kfGmxbjDBd5NigQ>? MmfPNU8zNjVizszN MYmyOEBp MmrxSG1UVw>? NE\mNIdz\WS3Y3XzJJRp\SCjY4TpeoF1cW:wIH;mJGFsfCCjbnSgdFcxWz[N MU[yNVkzPjl4NR?=
platelet  NV[5VVZuTnWwY4Tpc44hSXO|YYm= NUjYc5Z7OcLizszt MlXCOUBucW5? MnPKbY5pcWKrdIOgSoPPu1KLSVGtcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44> NIPNSm4zOTh2OE[5OC=>
platelet  NFr6NVNHfW6ldHnvckBCe3OjeR?= NHPyUFkxNjB3L{GvNk42KM7:TR?= NHLwSmk2KG2rbh?= NYTtWpROcW6qaXLpeJMhfGinIIPp[45idGmwZzDt[YNp[W6rc33zJIRwf26|dILlZY0hd2ZiRnROt3JKUUF? MX[yNVg1QDZ7NB?=
DoHH2 Ml7CRZBweHSxc3nzJGF{e2G7 Mk\ENE8{NzFyIN88US=> M2P6R|Q5KGh? NVzP[3dkcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MonKNlA5PzV2MEi=
Jeko-1  M2XWNGFxd3C2b4Ppd{BCe3OjeR?= NUXtVo5mOC9|L{GwJO69VQ>? M1Hmc|Q5KGh? Mn3LbY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? NVfhSIFOOjB6N{W0NFg>
Raji  NF25cJFCeG:ydH;zbZMhSXO|YYm= M2fON|AwOy9zMDFOwG0> NFn1U4U1QCCq NIXaU5dqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NYToeW1jOjB6N{W0NFg>
DHL4 Ml;oRZBweHSxc3nzJGF{e2G7 MlzlNE8yNzRizszN MXu5OkBp NVPYTGRFcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M1qyPVE5ODB4Nkm2
LY7 MofJRZBweHSxc3nzJGF{e2G7 NVS1T3JROC9zL{Sg{txO M1e3[Fk3KGh? NUPMZodbcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> Mly5NVgxODZ4OU[=
LY3 NWXDSJJtSXCxcITvd4l{KEG|c3H5 NHy4N|YxNzFxNDFOwG0> M{DTfVk3KGh? NHHDWlhqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NV\QTZVSOThyME[2PVY>
DHL6 M3u2bGFxd3C2b4Ppd{BCe3OjeR?= MoTwNE8yNzRizszN NUDzOWwzQTZiaB?= NV3welR[cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NH7mWFAyQDByNk[5Oi=>
LY10 MnLqRZBweHSxc3nzJGF{e2G7 M1\UOlAwOS92IN88US=> MUG5OkBp MXfpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnTvNVgxODZ4OU[=
DHL10 NFfhOIdCeG:ydH;zbZMhSXO|YYm= MlLFNE8yNzRizszN M{\mTFk3KGh? MoHMbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MljkNVgxODZ4OU[=
Wsu-NHL NInONIFCeG:ydH;zbZMhSXO|YYm= NF\BN48xNzFxNDFOwG0> Mn7rPVYhcA>? MX7pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NXLwO3J{OThyME[2PVY>
LY18 NHPDe5lCeG:ydH;zbZMhSXO|YYm= NH;hd4wxNzFxNDFOwG0> M1XpUVk3KGh? M3XqeYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M2rCdVE5ODB4Nkm2
LY1 MljhRZBweHSxc3nzJGF{e2G7 MkjQNE8yNzRizszN MnfsPVYhcA>? M1H1d4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1TmO|E5ODB4Nkm2
DHL8 MoTNRZBweHSxc3nzJGF{e2G7 M2XjOVAwOS92IN88US=> NYD2XmtoQTZiaB?= MYfpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MYGxPFAxPjZ7Nh?=
DHL4 MojjRZBweHSxc3nzJGF{e2G7 MoezOEDPxE1? MX25OkBp M1TyU4lv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NUix[5huOThyME[2PVY>
DHL6 M{\3RmFxd3C2b4Ppd{BCe3OjeR?= M33XdFQh|ryP MkHSPVYhcA>? NYTu[3hUcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MUOxPFAxPjZ7Nh?=
LY3 NGfnWHpCeG:ydH;zbZMhSXO|YYm= NXXo[WFTPCEQvF2= NYi3eWNKQTZiaB?= NWrGTYVxcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MUGxPFAxPjZ7Nh?=
LY7 MoKyRZBweHSxc3nzJGF{e2G7 NY\qdnZ1PCEQvF2= NHXaW4Q6PiCq MUXpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NFvKZYcyQDByNk[5Oi=>
DHL4 MYLGeY5kfGmxbjDBd5NigQ>? Mkf3OEDPxE1? Mo\HNVYhcA>? NHnXfm9qdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MmWwNVgxODZ4OU[=
LY7 NXH0eYRuTnWwY4Tpc44hSXO|YYm= NFjWTXU1KM7:TR?= MVOxOkBp MnnRbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NHriOZAyQDByNk[5Oi=>
LY3 NUDSWlI{TnWwY4Tpc44hSXO|YYm= MVO0JO69VQ>? MUixOkBp MWDpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NHfld|gyQDByNk[5Oi=>
DHL6 Mn;tSpVv[3Srb36gRZN{[Xl? M2W3TVQh|ryP MmLMNVYhcA>? MWnpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= Mle2NVgxODZ4OU[=
LY10 NGfNd2pHfW6ldHnvckBCe3OjeR?= NH\qco81KM7:TR?= MlL0NVYhcA>? MXrpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MnPrNVgxODZ4OU[=
Wsu-NHL NFi1NWFHfW6ldHnvckBCe3OjeR?= MXy0JO69VQ>? NGfrO2YyPiCq MlzpbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= MXmxPFAxPjZ7Nh?=
LY18 NGLhdnlHfW6ldHnvckBCe3OjeR?= M4HWVlQh|ryP M{G3ZlE3KGh? MVvpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MmfFNVgxODZ4OU[=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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):
30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.
30mg/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 Conditions Sponsor/Collaborators Start Date Phases
NCT01645085 Completed Healthy Volunteers AstraZeneca July 2012 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.

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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