R406

For research use only. Not for use in humans.

目录号：S2194

R406 Chemical Structure

CAS No. 841290-81-1

R406 是一种有效的 Syk 抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。R406 可诱导凋亡。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2341.19 现货
RMB 1421.87 现货
RMB 7119.85 现货
RMB 16298.1 现货
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客户使用Selleck生产的R406发表文献72篇：

产品安全说明书

Syk抑制剂选择性比较

生物活性

产品描述 R406 是一种有效的 Syk 抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。R406 可诱导凋亡。Phase 1。
特性 Rigel选择R406作为治疗风湿性关节炎的潜在领先药物。
靶点
Flt3 [1]
(Cell-free assay)		 Syk [1]
(Cell-free assay)
41 nM
体外研究

R406强抑制免疫球蛋白 E (IgE)和 IgG调节的受体信号活性。R406抑制IgE抗体诱导的 LTC4 ，细胞因子和趋化因子的产生和释放, 包括TNFα, IL-8, 和GM-CSF。R406 抑制肥大细胞中T细胞Syk底物链接蛋白的激活和B细胞中B细胞链接蛋白/SLP65的磷酸化作用。R406 结合到Syk的ATP结合袋中，抑制Syk的激酶活性， R406是ATP竞争性抑制剂，Ki为30 nM。R406阻断单核细胞/巨噬细胞和中性白细胞中Syk依赖的FcR调节活性，且阻断B淋巴细胞中BCR调节活性。[1]406 明显诱导慢性淋巴细胞白血病（CCL）细胞凋亡，且阻断CCL3和CCL4 分泌。[2] R406有效抑制血小板信号，且抑制使用特殊抗体或 HIT 病患的血浆通过FcγRIIA 交叉结合形成的功能。[4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
AMO-1 NEnDNIJHfW6ldHnvckBCe3OjeR?= MVexJO69VQ>? M1e5dlPDqGh? MVTy[YR2[2W|IH3p[5JifGmxbtMg MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ3MUe2NUc,OjZ{NUG3OlE9N2F-
U266 MYHGeY5kfGmxbjDBd5NigQ>? MorWNUDPxE1? MVSzxsBp NEezXohz\WS3Y3XzJI1q\3KjdHnvcuKh NXzpclV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yOVE4PjFpPkK2NlUyPzZzPD;hQi=>
Jeko-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml36OFghcA>? NEG4WFFKSzVyPUWuNFY5OjZizszN NHHpTlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOVc2PSd-MkW4N|U4PTV:L3G+
Mino MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPWOFghcA>? MWPJR|UxRTVwN{C4OVQh|ryP MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NUe1OUc,OjV6M{W3OVU9N2F-
Jeko-1 NEDzOGdCeG:ydH;zbZMhSXO|YYm= NHXHPYQ2yqEQvF2= MmD1NlQhcA>? NEfKXWpqdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz M{e0SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO1O|U2Lz5{NUizOVc2PTxxYU6=
primary MCL M1L4fGFxd3C2b4Ppd{BCe3OjeR?= M3\qWVIhyrWP NXvCVlZpOjRiaB?= MYXpcoNz\WG|ZYOgd4lodmmoaXPhcpRtgSCjcH;weI9{cXQEoB?= NH6zWWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO4PFM4Oyd-MkWzPFg{PzN:L3G+
PBMCs M1XQfWNmdGxiVnnhZoltcXS7IFHzd4F6 MmPRNE02OCEQvF2= M4DXPVI1KGh? NGLkb45FVVOR NYq4SWlWcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHXYZ2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyO|g3Oid-MkWxNlc5PjJ:L3G+
PBMCs M1rqbWZ2dmO2aX;uJGF{e2G7 M3W0RVUh|ryP M2C5dFEhcA>? NUG4Z44yTE2VTx?= M3q3cIRm[3KnYYPld{B1cGViY3XscEBucWe{YYTpc44> MljnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMke4OlIoRjJ3MUK3PFYzRC:jPh?=
CFSE-CD4+ T  NIPzNm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnpNE4xPjJ3LUGg{txO MoftOEBl MXnicI9kc3NicILvcIln\XKjdHnvckBw\iCJVljEMYRmemm4ZXSgR2Q1M8LiVDDj[YxteyCjbnSgR2QyOWJtwrDj[Yxtew>? NFLRZoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[3PVk5Oid-MkS2O|k6QDJ:L3G+
CFSE-CD11b+ NFTNVmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWmzU5JQOC5yNkK1MVEh|ryP M2nrRVgh\A>? NVPkTIw1[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= MnX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4N{m5PFIoRjJ2Nke5PVgzRC:jPh?=
HMECs M{DTUmZ2dmO2aX;uJGF{e2G7 MUmwMVExKM7:TR?= MYCyNEBucW5? MmG3bY5pcWKrdIOgWmVITi2|dHnteYxifGWmIILlcIVie2Vib3[gUm8> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN{OUW0OEc,OjR|Mkm1OFQ9N2F-
AB5 MYrBdI9xfG:|aYOgRZN{[Xl? MXKwMVIvPSEQvF2= NUH4OFMxPDhiaB?= MVzEUXNQ NELBXHdqdmS3Y3XzJIFxd3C2b4Ppdy=> MlvHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|OUi5NVEoRjJ|M{m4PVEyRC:jPh?=
JB7 NX72bGFiSXCxcITvd4l{KEG|c3H5 M1;NUlAuOi53IN88US=> NVvTZoVpPDhiaB?= MlvPSG1UVw>? M3\teIlv\HWlZYOgZZBweHSxc3nz MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OEmxNUc,OjN|OUi5NVE9N2F-
AB5 M{XFe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[5OJcxNTJwNTFOwG0> NVLyNYFHPDhiaB?= NWLHbGwzTE2VTx?= MWnpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OEmxNUc,OjN|OUi5NVE9N2F-
JB7 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDxNE0zNjVizszN MWC0PEBp MoX1SG1UVw>? NHfRXZhqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NWjDblR3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVg6OTFpPkKzN|k5QTFzPD;hQi=>
RL MVLGeY5kfGmxbjDBd5NigQ>? MkfkNk42NzVizszN NXPiVpZ3OjRxNEigbC=> M1O2S2ROW09? MkfkbY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? NXHEZXBqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlY6PjVpPkKxPVI3QTZ3PD;hQi=>
RL M4fMW2Z2dmO2aX;uJGF{e2G7 MnrpNU8zNjVizszN Ml;RNlQhcA>? NGPncolFVVOR MUny[YR2[2W|IITo[UBi[3SrdnH0bY9vKG:oIFHreEBidmRicEewV|ZM M3;xNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUK2PVY2Lz5{MUmyOlk3PTxxYU6=
platelet  MlS5SpVv[3Srb36gRZN{[Xl? NEP1[YsyyqEQvH2= MU[1JI1qdg>? MoLibY5pcWKrdIOgSoPPu1KLSVGtcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44> NXLL[Gh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG4OFg3QTRpPkKxPFQ5Pjl2PD;hQi=>
platelet  Mn;iSpVv[3Srb36gRZN{[Xl? MVSwMlA2NzFxMj61JO69VQ>? MmnqOUBucW5? M1\OcolvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC NH31Noc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi0PFY6PCd-MkG4OFg3QTR:L3G+
DoHH2 MmTMRZBweHSxc3nzJGF{e2G7 M2jVXVAwOy9zMDFOwG0> MY[0PEBp NFrzSHBqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= MkK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6N{W0NFgoRjJyOEe1OFA5RC:jPh?=
Jeko-1  NFfzTodCeG:ydH;zbZMhSXO|YYm= NV\ZeZFjOC9|L{GwJO69VQ>? M1fs[lQ5KGh? NXnSfphWcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= NXfXdplCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4O|U1ODhpPkKwPFc2PDB6PD;hQi=>
Raji  M3u5WWFxd3C2b4Ppd{BCe3OjeR?= NGL4[owxNzNxMUCg{txO MmHLOFghcA>? MmT0bY5lfWOnczDj[YxtKGSnYYToJJNq\26rZnnjZY51dHl? NEDCeJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi3OVQxQCd-MkC4O|U1ODh:L3G+
DHL4 MVjBdI9xfG:|aYOgRZN{[Xl? M3XvO|AwOS92IN88US=> M1TDd|k3KGh? NV;uUY1ScW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> Mln5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY7 NIPPOo9CeG:ydH;zbZMhSXO|YYm= MXKwM|EwPCEQvF2= NVr5c21FQTZiaB?= NGO2TW9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NEDsdYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
LY3 NHzZUVFCeG:ydH;zbZMhSXO|YYm= M3LWVlAwOS92IN88US=> NHXTd3Q6PiCq Mo\RbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= Mn7TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
DHL6 MmfFRZBweHSxc3nzJGF{e2G7 NXPNVI1{OC9zL{Sg{txO MUC5OkBp M{PUdolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY10 NXqydFF5SXCxcITvd4l{KEG|c3H5 MmrhNE8yNzRizszN MVW5OkBp M1nm[olv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M2H1WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL10 NVnTbo86SXCxcITvd4l{KEG|c3H5 MWmwM|EwPCEQvF2= M{f6dVk3KGh? MmnkbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NXHJSJE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
Wsu-NHL MoHFRZBweHSxc3nzJGF{e2G7 Mn:1NE8yNzRizszN MVq5OkBp M1;IOIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY18 NI\1TpFCeG:ydH;zbZMhSXO|YYm= NF:3d3gxNzFxNDFOwG0> NYLKOXRQQTZiaB?= M3TFPYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M4DIU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
LY1 MnKyRZBweHSxc3nzJGF{e2G7 NXXmcVZrOC9zL{Sg{txO MofCPVYhcA>? M{nRfolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NFTEbZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
DHL8 Mlz4RZBweHSxc3nzJGF{e2G7 NUSzeXk5OC9zL{Sg{txO Mki3PVYhcA>? MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NF[wZZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
DHL4 NXnvO3lZSXCxcITvd4l{KEG|c3H5 NIn3SIk1KM7:TR?= Ml34PVYhcA>? MlPvbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MmX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
DHL6 M1;QRmFxd3C2b4Ppd{BCe3OjeR?= NITpcGk1KM7:TR?= MWK5OkBp NHTW[HNqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY3 MUfBdI9xfG:|aYOgRZN{[Xl? NYjCXYFwPCEQvF2= NIOwVWY6PiCq NH\IdmpqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY7 MlTtRZBweHSxc3nzJGF{e2G7 NIjjc3Y1KM7:TR?= NGLOOYI6PiCq NIiwNJpqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 M2jIe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL4 M37LZ2Z2dmO2aX;uJGF{e2G7 M1;Ob|Qh|ryP MWWxOkBp M4C1eIlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NUHrTGg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY7 M2T1XmZ2dmO2aX;uJGF{e2G7 MlqwOEDPxE1? Mn\4NVYhcA>? Mmf2bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NHv2c2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
LY3 M{HBNWZ2dmO2aX;uJGF{e2G7 MWe0JO69VQ>? NVLufmRmOTZiaB?= MV3pcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
DHL6 NHTZdZBHfW6ldHnvckBCe3OjeR?= MUG0JO69VQ>? MU[xOkBp MorTbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NUXGVW83RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
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SK-M-MC M3\JWWZ2dmO2aX;uJIF{e2G7 NXvhUpZDOSCqch?= MkTVTY5pcWKrdHnvckBw\iCUZYSgbY4hcHWvYX6gV2suVS2PQzDj[YxteyCjc4Pld5Nm\CCjczDhd5Nme3OnZDDhd{BxcG:|cHjvdplt[XSrb36gZYZ1\XJiMTDodkBqdmO3YnH0bY9vNCCHQ{WwQVAvODN4zszNMi=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUWxOEc,OjR5N{m1NVQ9N2F-
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B-cells NY\4c|RKTnWwY4Tpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKFO\SzDpckBpfW2jbjDCMYNmdGy|IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBH[2Wyc3nsc45TOS:IY3fhcY1iWi2vZXTpZZRm\CC|aXfuZYxqdmdicnXzdI9ve2W|LDDFR|UxRTBwMES4{txONg>? Mn3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NUeyNVMoRjJ{MkW3NlE{RC:jPh?=
Ramos NFzSNXFHfW6ldHnvckBie3OjeR?= NYWxZndbUW6qaXLpeIlwdiCxZjDTfYshcW5iYX70bYh2dWGwIFnnUU1{fGmvdXzheIVlKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGJEWi2vZXTpZZRm\CCETF7LJJBpd3OyaH;yfYxifGmxbjDifUBk\WyudXzhdkBie3OjeTygSWM2OD1yLkC1N:69VS5? M1TFPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e5OVE1Lz5{NEe3PVUyPDxxYU6=
mesangial cells Mk\YSpVv[3Srb36gZZN{[Xl? M3Xhd2lvcGmkaYTpc44hd2ZiU2nLJIlvKGO3bIT1doVlKGi3bXHuJI1me2GwZ3nhcEBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iRnPldJNqdG:wUkGvSoNo[W2vYWKtcYVlcWG2ZXSgd4lodmGuaX7nJJJme3CxboPld{whTUN3ME2wMlA2Ps7:TT6= NWf3Zm1qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOVczOTNpPkKyNlU4OjF|PD;hQi=>
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B-cells NEfXT4RHfW6ldHnvckBie3OjeR?= MXixJIhz MlfmTY5pcWKrdHnvckBw\iCVeXugbY4h[WyyaHHJ[20ue3SrbYXsZZRm\CCqdX3hckBDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkAyKGi{IHnuZ5Vj[XSrb36gZpkh\myxdzDjfZRwdWW2comsJGVEPTB;MD6xOVHPxE1w NEXHSok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVUyPCd-MkS3O|k2OTR:L3G+
THP1 M4K2RWZ2dmO2aX;uJIF{e2G7 M1nzNmlvcGmkaYTpc44hd2ZiU2nLJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGZk\XC|aXzvcnIyN0[lZ3HtcYFTNW2nZHnheIVlKHOrZ37hcIlv\yC{ZYPwc45{\XNuIFXDOVA:OC5zN{JOwG0v M2LNPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkW3NlE{Lz5{MkK1O|IyOzxxYU6=
B-cells MojESpVv[3Srb36gZZN{[Xl? M3TudVEhcHJ? NHnjdIRKdmirYnn0bY9vKG:oIGP5b{BqdiCjbIDoZWloVS2|dHnteYxifGWmIHj1cYFvKEJiY3XscJMh[XO|ZYPz[YQh[XNiQ1S4OkBmgHC{ZYPzbY9vKGGodHXyJFEhcHJiaX7jeYJifGmxbjDifUBndG:5IHP5eI9u\XS{eTygSWM2OD1yLkOzOe69VS5? NV\z[HJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k2OTRpPkK0O|c6PTF2PD;hQi=>
Ramos M2\kVWZ2dmO2aX;uJIF{e2G7 MlfJTY5pcWKrdHnvckBw\iCVeXugbY4h[W62aTDJ[20ue3SrbYXsZZRm\CCqdX3hckBT[W2xczDj[YxteyCjc4Pld5Nm\CCjczDCUG5MKHCqb4PwbI9zgWyjdHnvckBjgSClZXzseYxieiCjc4PhfUwhUUN3ME2wMlQ2P87:TT6= NVKwNIdsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3NlY5ODZpPkK0O|I3QDB4PD;hQi=>
Rec1 Mn\DSpVv[3Srb36gZZN{[Xl? M2nJc|IvPSC3TR?= NVyzdGd3PiCqcoO= MYjJcohq[mm2aX;uJI9nKEKWSzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUnXjNUBk\WyuczDheEAzNjVidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> Ml\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MkK4O|coRjJ3MkKyPFc4RC:jPh?=
Rec1 MoCzSpVv[3Srb36gZZN{[Xl? NITsOo4zNjVidV2= M4[zdVYhcHK| NGW1XYVKdmirYnn0bY9vKG:oIGP5b{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gVoVkOSClZXzsd{BifCB{LkWgeW0hcW6ldXLheIVlKG[xcjC2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIH3leIhw\A>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{Mki3O{c,OjV{MkK4O|c9N2F-
Rec1 M37oV2Z2dmO2aX;uJIF{e2G7 NHGwcGszNjVidV2= M3TZcVYhcHK| M1vQTmlvcGmkaYTpc44hd2ZiTInuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDS[YMyKGOnbHzzJIF1KDJwNTD1UUBqdmO3YnH0[YQh\m:{IE[gbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l NEfvPIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyNlg4Pyd-MkWyNlI5Pzd:L3G+
SJ-GBM2 M4XMTJFJXFNiYYPzZZk> NG\1bHRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NIq2VIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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NB-EBc1 NVyzbGZIeUiWUzDhd5NigQ>? NF7wRodyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MnPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MXjxTHRUKGG|c3H5 NFXmNnNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MoD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NXHPRWZPeUiWUzDhd5NigQ>? MVXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| M3TTW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 Ml7GdWhVWyCjc4PhfS=> NFK4UWtyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= M1fQcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... 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
体内研究 在已经预防处理的鼠内进行阳性Arthus 反应，5 mg/kg R406诱导鼠皮肤病变达到86%。R406作用于抗体诱导的关节炎鼠模型，也有效抑制炎症。[1] 自身免疫反应时，R406不会影响巨噬细胞和嗜中性粒细胞的功能，免疫毒性为最低水平。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验：[1]
- 合并
  • Animal Models: 在C57BL/6鼠中腹腔注射150 μL 取自成年K/BxN鼠的混合血清诱导产生关节炎。
  • Dosages: 1 或5 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (159.07 mM)
Water Insoluble
Ethanol 0 mg/mL (0.0 mM)
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
5%dmso+95%cornoil
 6mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 628.63
化学式

C22H23FN6O5.C6H6O3S
CAS号 841290-81-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01598571 Completed Drug: Fostamatinib Healthy AstraZeneca May 2012 Phase 1
NCT01387308 Completed Drug: Fostamatinib Healthy AstraZeneca August 2011 Phase 1
NCT01336218 Completed Drug: fostamatinib|Drug: rifampicin Rheumatoid Arthritis|Healthy Volunteers AstraZeneca April 2011 Phase 1
NCT01222455 Completed Drug: Fostamatinib Hepatic Impairment|Healthy Volunteers|Pharmacokinetics|Amount of R406 in Blood AstraZeneca October 2010 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    What’s the difference between S1533 and S2194?

  • 回答：

    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.

Selleck产品目录册

Syk Signaling Pathway Map

Syk Inhibitors with Unique Features

相关Syk产品

  • PX-478 2HCl New

    PX-478 2HCl 是一种具有口服活性的选择性hypoxia-inducible factor-1α (HIF-1α)抑制剂。PX-478 2HCl可诱导凋亡并具有抗肿瘤的活性。Phase 1。

  • Defactinib (VS-6063) New

    Defactinib (VS-6063, PF-04554878)是一种选择性，且口服有效的FAK抑制剂。Phase 2。

  • SU6656 New

    SU 6656 是一种选择性 Src 家族激酶抑制剂，对Src，Yes，Lyn，和 Fyn 的 IC50 分别为 280 nM，20 nM，130 nM，和 170 nM。

  • R406 (free base)

    R406 (free base) 是一种有效的Syk抑制剂，无细胞试验中IC50为41 nM，强效抑制Syk而不能抑制Lyn，对Flt3作用效果低5倍。R406 (free base) 可触发凋亡。Phase 1。

  • Fostamatinib (R788) disodium

    Fostamatinib disodium (R788, Tamatinib Fosdium)是活性代谢物R406的前体药物，是一种Syk抑制剂，无细胞试验中IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果弱5倍。Phase 3。

    Features:R935788是临床上常用的药物前体 R406的口服试剂, 在药物性能上优于R406，具有较高的溶解度和生物利用度。

  • Fostamatinib (R788)

    Fostamatinib (R788)是活性代谢产物R406的前体药物，是一种Syk抑制剂，IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果低5倍。Phase 3。

    Features:Converted into its active metabolite R406 in vivo.

  • Piceatannol

    Piceatannol，是一种天然二苯乙烯，是选择性Syk抑制剂，比作用于Lyn选择性高10倍左右。

  • PRT062607 (P505-15) HCl

    PRT062607 (P505-15, BIIB057, PRT-2607)是一种新型的，高度选择性Syk抑制剂，无细胞试验中IC50为1 nM，作用于Syk比作用于Fgr，PAK5，Lyn，FAK，Pyk2, FLT3, MLK1 和Zap70选择性高80倍以上。

  • Entospletinib (GS-9973)

    Entospletinib (GS-9973)是一种口服具有生物活性的，选择性Syk抑制剂，无细胞试验中IC50为7.7 nM。在细胞中，对Syk的选择性比对其他激酶（如Jak2, ckit, Flt3, Ret, KDR）高13-1000倍。

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765)是一种有效的，高选择性的Brutons tyrosine kinase (Btk)抑制剂，无细胞试验中IC50为0.5 nM，对Bmx， CSK， FGR， BRK及HCK适度有效，对EGFR， Yes， ErbB2， JAK3等作用效果较弱。Ibrutinib 可作为Btk配体用于合成包括P13I在内的一系列PROTAC。

Tags: 购买R406 | R406供应商 | 采购R406 | R406价格 | R406生产 | 订购R406 | R406代理商
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID