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76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 MmnnSpVv[3Srb36gRZN{[Xl? M1;rOVEh|ryP M1HIU|PDqGh? MoT4doVlfWOnczDtbYdz[XSrb39CpC=> NH\RfWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK1NVc3OSd-Mk[yOVE4PjF:L3G+
U266 MVLGeY5kfGmxbjDBd5NigQ>? MkHrNUDPxE1? NG\tW5A{yqCq NX20OIt5emWmdXPld{BucWe{YYTpc47DqA>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ3MUe2NUc,OjZ{NUG3OlE9N2F-
Jeko-1 M4r0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkThOFghcA>? NYe0VnBvUUN3ME21MlA3QDJ4IN88US=> NWrheIQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|U4PTVpPkK1PFM2PzV3PD;hQi=>
Mino M1XsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXKN281QCCq M2\EeGlEPTB;NT63NFg2PCEQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NUe1OUc,OjV6M{W3OVU9N2F-
Jeko-1 MmrxRZBweHSxc3nzJGF{e2G7 NEjMems2yqEQvF2= NWXCWJVROjRiaB?= MWnpcoR2[2W|IEK1MlHDqMLzwrCzMlLDqCViYYDvdJRwe2m| NEPjd2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOVc2PSd-MkW4N|U4PTV:L3G+
primary MCL NEL3PIpCeG:ydH;zbZMhSXO|YYm= NU\sW|RJOiEEtV2= MYGyOEBp MV7pcoNz\WG|ZYOgd4lodmmoaXPhcpRtgSCjcH;weI9{cXQEoB?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN6OEO3N{c,OjV|OEizO|M9N2F-
PBMCs MoDzR4VtdCCYaXHibYxqfHliQYPzZZk> NXfr[IdZOC13MDFOwG0> NVnDN5h6OjRiaB?= NYLKSXc6TE2VTx?= MnfrbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{N{i2Nkc,OjVzMke4OlI9N2F-
PBMCs MkHCSpVv[3Srb36gRZN{[Xl? M1nuUlUh|ryP Ml;hNUBp MWrEUXNQ MV7k[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u M{fYd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK3PFYzLz5{NUGyO|g3OjxxYU6=
CFSE-CD4+ T  M4G0XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3ve4QxNjB4MkWtNUDPxE1? Mm\DOEBl M1\Q[IJtd2OtczDwdo9tcW[ncnH0bY9vKG:oIFfWTGQu\GW{aY\l[EBETDRtwrDUJINmdGy|IHHu[EBETDFzYjxCpINmdGy| M2\pbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nke5PVgzLz5{NE[3PVk5OjxxYU6=
CFSE-CD11b+ M2nFfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnrNE4xPjJ3LUGg{txO M4DWVVgh\A>? NVHyNldu[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= NGnkc|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[3PVk5Oid-MkS2O|k6QDJ:L3G+
HMECs MYTGeY5kfGmxbjDBd5NigQ>? NWG0fHo4OC1zMDFOwG0> NFXke2wzOCCvaX6= NWHCNFBmcW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? M4jBZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{K5OVQ1Lz5{NEOyPVU1PDxxYU6=
AB5 MWHBdI9xfG:|aYOgRZN{[Xl? MWqwMVIvPSEQvF2= NXXISok1PDhiaB?= MmPuSG1UVw>? Mk\GbY5lfWOnczDhdI9xfG:|aYO= NUPiPI1qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVg6OTFpPkKzN|k5QTFzPD;hQi=>
JB7 Ml\GRZBweHSxc3nzJGF{e2G7 NGLLN|kxNTJwNTFOwG0> MUi0PEBp M4[0OmROW09? NXHwOIx[cW6mdXPld{BieG:ydH;zbZM> NY\PNndTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVg6OTFpPkKzN|k5QTFzPD;hQi=>
AB5 NUHwOIpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2wMVIvPSEQvF2= Mmn4OFghcA>? NGHLWpBFVVOR MmXKbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M4\OSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m4PVEyLz5{M{O5PFkyOTxxYU6=
JB7 MkS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XwcVAuOi53IN88US=> NWDPS|FCPDhiaB?= MYDEUXNQ NUnnNGdJcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OEmxNUc,OjN|OUi5NVE9N2F-
RL M4\QfGZ2dmO2aX;uJGF{e2G7 NH74UnIzNjVxNTFOwG0> NVLh[VV1OjRxNEigbC=> M{fDdGROW09? MUDpcoR2[2W|IHGgdI91\W62IHTlZ5Jm[XOnIHnuJG1OWC17IH3SUmEh\XiycnXzd4lwdg>? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{Nkm2OUc,OjF7Mk[5OlU9N2F-
RL MlvjSpVv[3Srb36gRZN{[Xl? MlzoNU8zNjVizszN MYOyOEBp NX3DN4J3TE2VTx?= NUTpVYJxemWmdXPld{B1cGViYXP0bZZifGmxbjDv[kBCc3RiYX7kJJA4OFN4Sx?= NFTNRZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlk3PSd-MkG5NlY6PjV:L3G+
platelet  MoGxSpVv[3Srb36gRZN{[Xl? MnHxNeKh|ryv MnfmOUBucW5? MmH2bY5pcWKrdIOgSoPPu1KLSVGtcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44> NHPvSms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi0PFY6PCd-MkG4OFg3QTR:L3G+
platelet  NHTWUnFHfW6ldHnvckBCe3OjeR?= M2ftXFAvODVxMT:yMlUh|ryP M1zmSVUhdWmw MXXpcohq[mm2czD0bIUhe2mpbnHsbY5oKG2nY3jhcol{dXNiZH;3cpN1emWjbTDv[kBH[87|UlnJRS=> NXjOO21GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG4OFg3QTRpPkKxPFQ5Pjl2PD;hQi=>
DoHH2 M4\kPWFxd3C2b4Ppd{BCe3OjeR?= NUTjbVZ4OC9|L{GwJO69VQ>? MVq0PEBp NGnHW4NqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= M3XtRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEe1OFA5Lz5{MEi3OVQxQDxxYU6=
Jeko-1  M4rmOGFxd3C2b4Ppd{BCe3OjeR?= NF7PNlcxNzNxMUCg{txO M4TPZVQ5KGh? NF7nU3BqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NX;DTG1mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4O|U1ODhpPkKwPFc2PDB6PD;hQi=>
Raji  NEf3WlRCeG:ydH;zbZMhSXO|YYm= NWr6[oJjOC9|L{GwJO69VQ>? MUm0PEBp NFyxOZBqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= NWKyb3gxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4O|U1ODhpPkKwPFc2PDB6PD;hQi=>
DHL4 MVrBdI9xfG:|aYOgRZN{[Xl? M17G[VAwOS92IN88US=> M4TzXFk3KGh? NVzNXoRqcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M3LhTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
LY7 NXnNemhqSXCxcITvd4l{KEG|c3H5 M{PHblAwOS92IN88US=> MnzOPVYhcA>? MojPbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDByNk[5Okc,OThyME[2PVY9N2F-
LY3 NHPMO2pCeG:ydH;zbZMhSXO|YYm= NXTFWY02OC9zL{Sg{txO M3TwZlk3KGh? MYTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NEjBUJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
DHL6 NUDGO5B1SXCxcITvd4l{KEG|c3H5 NXrudYc6OC9zL{Sg{txO NF3aO|c6PiCq NYj1R3ZpcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MorZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY10 Ml\oRZBweHSxc3nzJGF{e2G7 MkXaNE8yNzRizszN MmTxPVYhcA>? NY\yOoNDcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M2XNPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL10 NF7wc|BCeG:ydH;zbZMhSXO|YYm= MnzJNE8yNzRizszN M1vxR|k3KGh? NYe3[YptcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NIXwS5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
Wsu-NHL MVXBdI9xfG:|aYOgRZN{[Xl? NYWz[WFWOC9zL{Sg{txO MnvQPVYhcA>? MUPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NXXRWHh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNFY3QTZpPkG4NFA3Pjl4PD;hQi=>
LY18 M4jEOGFxd3C2b4Ppd{BCe3OjeR?= MU[wM|EwPCEQvF2= NGrIZoo6PiCq MlH1bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MnXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY1 MmLHRZBweHSxc3nzJGF{e2G7 MkTaNE8yNzRizszN NWXwUYF6QTZiaB?= NH7UcYpqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MlzCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
DHL8 M1fySGFxd3C2b4Ppd{BCe3OjeR?= M4L3TlAwOS92IN88US=> MV:5OkBp Mo[xbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NIrKe5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
DHL4 NIHm[nJCeG:ydH;zbZMhSXO|YYm= M4DwVlQh|ryP MYC5OkBp Ml\ibY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> MlTwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
DHL6 M4DvcmFxd3C2b4Ppd{BCe3OjeR?= NUTkWJF{PCEQvF2= NVL4SnZ[QTZiaB?= NYPqfZIzcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? MmTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY3 NHnWSY9CeG:ydH;zbZMhSXO|YYm= MUi0JO69VQ>? MWG5OkBp NImwclZqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 MmTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY7 MV7BdI9xfG:|aYOgRZN{[Xl? MVW0JO69VQ>? MlfhPVYhcA>? NW\nXW9pcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? M1eyWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL4 M2LkS2Z2dmO2aX;uJGF{e2G7 M1LMblQh|ryP Mkj6NVYhcA>? NUPXNINqcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> Mle1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
LY7 M4XE[GZ2dmO2aX;uJGF{e2G7 M2rxVVQh|ryP NWq1eW95OTZiaB?= NIjxU2FqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NHuxUmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECwOlY6Pid-MUiwNFY3QTZ:L3G+
LY3 NWLE[mdETnWwY4Tpc44hSXO|YYm= MlnWOEDPxE1? M1nwW|E3KGh? MlPWbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= M1qyR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEC2Olk3Lz5zOECwOlY6PjxxYU6=
DHL6 NFr3TWJHfW6ldHnvckBCe3OjeR?= M1TkSVQh|ryP MUOxOkBp M4XQXYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MnTKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyME[2PVYoRjF6MEC2Olk3RC:jPh?=
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neutrophils MVTGeY5kfGmxbjDhd5NigQ>? NHG1W4xKdmirYnn0bY9vKG:oIGPZT{BqdiCqdX3hckBv\XW2cn;wbIlteyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gSoNmeHOrbH;uVlEwTmOpYX3tZXIudWWmaXH0[YQhe2mpbnHsbY5oKHKnc4DvcpNmeyxiRVO1NF0xNjB|M988UU4> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ3N{KxN{c,OjJ{NUeyNVM9N2F-
SK-M-MC MmHJSpVv[3Srb36gZZN{[Xl? MYCxJIhz M4jMVmlvcGmkaYTpc44hd2ZiUnX0JIlvKGi3bXHuJHNMNU1vTVOgZ4VtdHNiYYPz[ZN{\WRiYYOgZZN{\XO|ZXSgZZMheGixc4Doc5J6dGG2aX;uJIFnfGW{IEGgbJIhcW6ldXLheIlwdixiRVO1NF0xNjB|Nt88UU4> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUWxOEc,OjR5N{m1NVQ9N2F-
mast cells NXvKRmJITnWwY4Tpc44h[XO|YYm= M{OwT|EhcHJ? M1rOR2lvcGmkaYTpc44hd2ZiY1vpeEBqdiC|dHXtJINmdGxiZnHjeI9zNXO2aX31cIF1\WRiYn;u[UBu[XK{b4eg[IVzcX[nZDDtc5V{\SCvYYP0JINmdGy|IHHzd4V{e2WmIHHzJJBpd3OyaH;yfYxifGmxbjDh[pRmeiBzIHjyJIlv[3WkYYTpc44tKEWFNUC9NE4xPDcQvF2u MkjZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=
B-cells NV3pZ4hCTnWwY4Tpc44h[XO|YYm= NWXwcWRkUW6qaXLpeIlwdiCxZjDTXWshcW5iaIXtZY4hSi2lZXzsd{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iRnPldJNqdG:wUkGvSoNo[W2vYWKtcYVlcWG2ZXSgd4lodmGuaX7nJJJme3CxboPld{whTUN3ME2wMlA1QM7:TT6= NYXXWY86RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOVczOTNpPkKyNlU4OjF|PD;hQi=>
Ramos M3;uTmZ2dmO2aX;uJIF{e2G7 M3jnbmlvcGmkaYTpc44hd2ZiU4nrJIlvKGGwdHnoeY1idiCLZ12td5RqdXWuYYTl[EBpfW2jbjDSZY1weyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDCR3IudWWmaXH0[YQhSkyQSzDwbI9{eGixconsZZRqd25iYomgZ4VtdHWuYYKgZZN{[XluIFXDOVA:OC5yNUROwG0v NUDzd49VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k2OTRpPkK0O|c6PTF2PD;hQi=>
mesangial cells MY\GeY5kfGmxbjDhd5NigQ>? NHrMOFBKdmirYnn0bY9vKG:oIGPZT{BqdiCldXz0eZJm\CCqdX3hckBu\XOjbnfpZYwh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIF\j[ZB{cWyxbmKxM2Zk\2GvbXHSMY1m\GmjdHXkJJNq\26jbHnu[{Bz\XOyb37z[ZMtKEWFNUC9NE4xPTcQvF2u M4S3bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkW3NlE{Lz5{MkK1O|IyOzxxYU6=
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mouse bone marrow cells MVnGeY5kfGmxbjDhd5NigQ>? M37XcGlvcGmkaYTpc44hd2ZiSVyzJIRmeGWwZHXueEBxem:uaX\ldoF1cW:wIHnuJGM2Py:EMU[gcY92e2ViYn;u[UBu[XK{b4egZ4VtdHNidYPpcochYzOKXYTofY1q\GmwZTDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NF0xNjF2N988UU4> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd{NkiwOkc,OjR5Mk[4NFY9N2F-
B-cells MmD3SpVv[3Srb36gZZN{[Xl? NUjvR5VDOSCqch?= MlnvTY5pcWKrdHnvckBw\iCVeXugbY4h[WyyaHHJ[20ue3SrbYXsZZRm\CCqdX3hckBDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkAyKGi{IHnuZ5Vj[XSrb36gZpkh\myxdzDjfZRwdWW2comsJGVEPTB;MD6xOVHPxE1w Mm\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=
THP1 M2\3RmZ2dmO2aX;uJIF{e2G7 M2[zUWlvcGmkaYTpc44hd2ZiU2nLJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGZk\XC|aXzvcnIyN0[lZ3HtcYFTNW2nZHnheIVlKHOrZ37hcIlv\yC{ZYPwc45{\XNuIFXDOVA:OC5zN{JOwG0v MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ3N{KxN{c,OjJ{NUeyNVM9N2F-
B-cells M13O[WZ2dmO2aX;uJIF{e2G7 NVuyTGJ6OSCqch?= M1rodmlvcGmkaYTpc44hd2ZiU4nrJIlvKGGucHjhTYdONXO2aX31cIF1\WRiaIXtZY4hSiClZXzsd{Bie3Onc4Pl[EBieyCFREi2JIV5eHKnc4Ppc44h[W[2ZYKgNUBpeiCrbnP1ZoF1cW:wIHL5JIZtd3diY4n0c41mfHK7LDDFR|UxRTBwM{O1{txONg>? NXrVdWxxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k2OTRpPkK0O|c6PTF2PD;hQi=>
Ramos MonJSpVv[3Srb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKFO7azDpckBidnSrIFnnUU1{fGmvdXzheIVlKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IFLMUmsheGixc4Doc5J6dGG2aX;uJIJ6KGOnbHz1cIFzKGG|c3H5MEBKSzVyPUCuOFU4|ryPLh?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd{NkiwOkc,OjR5Mk[4NFY9N2F-
Rec1 MkHHSpVv[3Srb36gZZN{[Xl? NX3vZ2xSOi53IIXN NWm1b2NUPiCqcoO= MmHuTY5pcWKrdHnvckBw\iCEVFugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{Mki3O{c,OjV{MkK4O|c9N2F-
Rec1 MYTGeY5kfGmxbjDhd5NigQ>? NH[5fokzNjVidV2= M1fTdlYhcHK| MkX6TY5pcWKrdHnvckBw\iCVeXugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> NEnuO209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyNlg4Pyd-MkWyNlI5Pzd:L3G+
Rec1 MWjGeY5kfGmxbjDhd5NigQ>? NEjZSHIzNjVidV2= M4G5WlYhcHK| MYfJcohq[mm2aX;uJI9nKEy7bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUnXjNUBk\WyuczDheEAzNjVidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> M3HyU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkKyPFc4Lz5{NUKyNlg4PzxxYU6=
SJ-GBM2 NIfjTJNyUFSVIHHzd4F6 NXHqeHIxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> Mmj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 NYizcY9{eUiWUzDhd5NigQ>? NVjDRVNQeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MV3xTHRUKGG|c3H5 MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MmjOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 M3\BZZFJXFNiYYPzZZk> M{DCW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 MYXxTHRUKGG|c3H5 NVrYTm92eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MofhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NVfPeoJ[eUiWUzDhd5NigQ>? NGrlbJhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz M2n6XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NWXZfGlQeUiWUzDhd5NigQ>? MmDUdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? M13LcFxiKHSjcnfleF0oZ2KuYX7rK{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
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
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

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.

Syk Signaling Pathway Map

Syk Inhibitors with Unique Features

相关Syk产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID