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 2207.88 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55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 M3PGZ2Z2dmO2aX;uJGF{e2G7 M16ye|Eh|ryP MlnwN:KhcA>? M1;WNJJm\HWlZYOgcYloemG2aX;uxsA> NGHEclQzPjJ3MUe2NS=>
U266 M3X1VWZ2dmO2aX;uJGF{e2G7 MkDFNUDPxE1? NVu3ZnVXO8LiaB?= NIn2[2Fz\WS3Y3XzJI1q\3KjdHnvcuKh M4C1cFI3OjVzN{[x
Jeko-1 MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrPOFghcA>? M{i2ZWlEPTB;NT6wOlgzPiEQvF2= NVjBUGIzOjV6M{W3OVU>
Mino MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPmUm5MPDhiaB?= M3fafGlEPTB;NT63NFg2PCEQvF2= NFfub4wzPTh|NUe1OS=>
Jeko-1 NYqxT3BGSXCxcITvd4l{KEG|c3H5 MmjmOeKh|ryP MX:yOEBp NELSNmZqdmS3Y3XzJFI2NjIEoNMxxsA{NjMEoDWgZZBweHSxc3nz NXzpTIx{OjV6M{W3OVU>
primary MCL MXHBdI9xfG:|aYOgRZN{[Xl? NWfOWG1HOiEEtV2= NFjrXG8zPCCq MmrjbY5kemWjc3XzJJNq\26rZnnjZY51dHliYYDvdJRwe2m|wrC= M1jv[|I2Ozh6M{ez
PBMCs NFHoRVlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXjZdoN1OC13MDFOwG0> NVnuN5lsOjRiaB?= MlnnSG1UVw>? MWDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MlrJNlUyOjd6NkK=
PBMCs MonYSpVv[3Srb36gRZN{[Xl? MVS1JO69VQ>? M2PuWFEhcA>? MkDBSG1UVw>? MXjk[YNz\WG|ZYOgeIhmKGOnbHygcYloemG2aX;u NVewS2ZsOjVzMke4OlI>
CFSE-CD4+ T  NUDqOVVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnaNE4xPjJ3LUGg{txO MkHjOEBl MoDCZoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? MnS4NlQ3Pzl7OEK=
CFSE-CD11b+ NX\3TXRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rlXVAvODZ{NT2xJO69VQ>? MnjyPEBl NWDRbmlF[myxY3vzJJBzd2yrZnXyZZRqd25ib3[gS3ZJTC2mZYLpeoVlKEOGNDxCpHQh[2WubIOgZY5lKEOGMUHiL:Kh[2WubIO= NX7Bbo1EOjR4N{m5PFI>
HMECs M3vvdWZ2dmO2aX;uJGF{e2G7 NVrIdZF3OC1zMDFOwG0> MmjBNlAhdWmw NWHLXnJ4cW6qaXLpeJMhXkWJRj3zeIlufWyjdHXkJJJmdGWjc3Wgc4YhVk9? M4HJUlI1OzJ7NUS0
AB5 NWjyNIFqSXCxcITvd4l{KEG|c3H5 MV2wMVIvPSEQvF2= M4PtOFQ5KGh? MVjEUXNQ Ml7KbY5lfWOnczDhdI9xfG:|aYO= M2rLbVI{Ozl6OUGx
JB7 NVXCTI5XSXCxcITvd4l{KEG|c3H5 NFzMNFMxNTJwNTFOwG0> NUW2PZBpPDhiaB?= NFzCeXhFVVOR MVXpcoR2[2W|IHHwc5B1d3Orcx?= M{jTZVI{Ozl6OUGx
AB5 NGOycnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLjeXc2OC1{LkWg{txO MWm0PEBp MYDEUXNQ M33UOolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHzzfYMzOzN7OEmxNS=>
JB7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTlb4ZROC1{LkWg{txO M4LwOlQ5KGh? M1P5b2ROW09? NV34cGFrcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MVyyN|M6QDlzMR?=
RL M3PQbmZ2dmO2aX;uJGF{e2G7 M{fRe|IvPS93IN88US=> MXeyOE81QCCq Ml24SG1UVw>? MoDVbY5lfWOnczDhJJBwfGWwdDDk[YNz\WG|ZTDpckBOVVBvOTDtVm5CKGW6cILld5Nqd25? NX3BVGFsOjF7Mk[5OlU>
RL NFqwepRHfW6ldHnvckBCe3OjeR?= NVPyfm5NOS9{LkWg{txO NETOVG0zPCCq NELUZldFVVOR NWTrUoF1emWmdXPld{B1cGViYXP0bZZifGmxbjDv[kBCc3RiYX7kJJA4OFN4Sx?= MnHRNlE6OjZ7NkW=
platelet  MYDGeY5kfGmxbjDBd5NigQ>? NVPIXmFmOcLizszt NFewPIo2KG2rbh?= MXrpcohq[mm2czDGZ:6{WkmLQT3t[YRq[XSnZDDwcIF1\WyndDDh[4dz\WejdHnvci=> NIL5NnAzOTh2OE[5OC=>
platelet  Mk\lSpVv[3Srb36gRZN{[Xl? MYKwMlA2NzFxMj61JO69VQ>? MVK1JI1qdg>? M1fDSolvcGmkaYTzJJRp\SC|aXfuZYxqdmdibXXjbIFvcXOvczDkc5dve3S{ZXHtJI9nKE[lzsPSTWlC M2f3U|IyQDR6Nkm0
DoHH2 NEfwOlRCeG:ydH;zbZMhSXO|YYm= MWewM|MwOTBizszN NHriNWM1QCCq NE[5NVlqdmS3Y3XzJINmdGxiZHXheIghe2mpbnnmbYNidnSueR?= M3vjO|IxQDd3NEC4
Jeko-1  Mn;lRZBweHSxc3nzJGF{e2G7 Ml\ZNE8{NzFyIN88US=> NInKc3A1QCCq NX\zWHRucW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= M4DHVVIxQDd3NEC4
Raji  NYTMUXZySXCxcITvd4l{KEG|c3H5 MkHaNE8{NzFyIN88US=> M33pSVQ5KGh? M1vnfYlv\HWlZYOgZ4VtdCCmZXH0bEB{cWewaX\pZ4FvfGy7 NYr5UmRZOjB6N{W0NFg>
DHL4 NH;Gd5FCeG:ydH;zbZMhSXO|YYm= MWewM|EwPCEQvF2= NHnPelI6PiCq NX3mOIJ5cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MUSxPFAxPjZ7Nh?=
LY7 M4rjZ2Fxd3C2b4Ppd{BCe3OjeR?= NVrjbFN{OC9zL{Sg{txO NFTvVlI6PiCq M{nvT4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NV7SNZlLOThyME[2PVY>
LY3 NWOyTHdwSXCxcITvd4l{KEG|c3H5 NH7ScVQxNzFxNDFOwG0> MUK5OkBp MW\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M3TRVVE5ODB4Nkm2
DHL6 MWrBdI9xfG:|aYOgRZN{[Xl? MmfiNE8yNzRizszN NFO4eIg6PiCq MX\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MmPzNVgxODZ4OU[=
LY10 Mlm4RZBweHSxc3nzJGF{e2G7 NYnJXmFCOC9zL{Sg{txO MnzYPVYhcA>? NXH5NGhwcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MWCxPFAxPjZ7Nh?=
DHL10 NWLxNFlRSXCxcITvd4l{KEG|c3H5 MVGwM|EwPCEQvF2= MUS5OkBp MkTqbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NF30SocyQDByNk[5Oi=>
Wsu-NHL NHKz[HhCeG:ydH;zbZMhSXO|YYm= NH[yZXcxNzFxNDFOwG0> NVfwUGd6QTZiaB?= MoL3bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NIHvfY8yQDByNk[5Oi=>
LY18 NY[zd5Q4SXCxcITvd4l{KEG|c3H5 NULMbJU3OC9zL{Sg{txO MV[5OkBp NF\yTHRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MkXLNVgxODZ4OU[=
LY1 M1nGfmFxd3C2b4Ppd{BCe3OjeR?= MXOwM|EwPCEQvF2= NWTtOIlUQTZiaB?= MXfpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnPlNVgxODZ4OU[=
DHL8 Ml\SRZBweHSxc3nzJGF{e2G7 MoW3NE8yNzRizszN MX65OkBp NHX1OItqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NV33NldzOThyME[2PVY>
DHL4 NFHUUpJCeG:ydH;zbZMhSXO|YYm= MVi0JO69VQ>? NGXlZ|M6PiCq MoXUbY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> NXnadHNzOThyME[2PVY>
DHL6 M4TkO2Fxd3C2b4Ppd{BCe3OjeR?= MYi0JO69VQ>? MYK5OkBp NWDXXnQ1cW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? NG\jNnIyQDByNk[5Oi=>
LY3 MXzBdI9xfG:|aYOgRZN{[Xl? NIfiWVQ1KM7:TR?= MXS5OkBp NUjCfZlPcW6mdXPld{BkdGWjdnHn[UBw\iClYYPwZZNmeyB7IHHu[EA{NCCkdYSgco91KGOjc4Dhd4UhQA>? NYPM[XdpOThyME[2PVY>
LY7 NUXCd|dmSXCxcITvd4l{KEG|c3H5 NH3rdZk1KM7:TR?= NGDLdFU6PiCq MVLpcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NEHzWoMyQDByNk[5Oi=>
DHL4 MkDWSpVv[3Srb36gRZN{[Xl? MlvGOEDPxE1? M1iw[FE3KGh? M1jzTYlvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u Mk\lNVgxODZ4OU[=
LY7 NUDNV2ZQTnWwY4Tpc44hSXO|YYm= NXXhfmdtPCEQvF2= MUKxOkBp MmPmbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NIfNOpMyQDByNk[5Oi=>
LY3 MkL2SpVv[3Srb36gRZN{[Xl? MXe0JO69VQ>? MXuxOkBp Mm[zbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NVW5bo03OThyME[2PVY>
DHL6 NXjmZ2dKTnWwY4Tpc44hSXO|YYm= NVWzc29OPCEQvF2= MkHXNVYhcA>? MnP6bY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NYXLe|NiOThyME[2PVY>
LY10 Ml7HSpVv[3Srb36gRZN{[Xl? NEDm[Iw1KM7:TR?= M1K1TFE3KGh? NVjwdI9ocW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> NXzhTHFSOThyME[2PVY>
Wsu-NHL M4m4SmZ2dmO2aX;uJGF{e2G7 M{XaTlQh|ryP MWSxOkBp M3\IRolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u MkXzNVgxODZ4OU[=
LY18 M4nPS2Z2dmO2aX;uJGF{e2G7 NYHwZYt2PCEQvF2= M{jpOlE3KGh? MWjpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NGfkR|gyQDByNk[5Oi=>

... 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、MSDS / 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、MSDS / 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