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 984.61 现货
RMB 1421.87 现货
RMB 2207.88 现货
RMB 7119.85 现货
RMB 16298.1 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的R406发表文献49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 NGL4UVVHfW6ldHnvckBCe3OjeR?= NIjsV4UyKM7:TR?= MVOzxsBp NXHTOGtOemWmdXPld{BucWe{YYTpc47DqA>? NXu3Tm15OjZ{NUG3OlE>
U266 NYH6VWR1TnWwY4Tpc44hSXO|YYm= MV[xJO69VQ>? M3fNVVPDqGh? NIHVfmFz\WS3Y3XzJI1q\3KjdHnvcuKh MljwNlYzPTF5NkG=
Jeko-1 NYrUOFRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInVO4c1QCCq NX;iUXRuUUN3ME21MlA3QDJ4IN88US=> Mmm0NlU5OzV5NUW=
Mino Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:2WlY1QCCq M4XFPWlEPTB;NT63NFg2PCEQvF2= Mo\HNlU5OzV5NUW=
Jeko-1 M3X0SmFxd3C2b4Ppd{BCe3OjeR?= M3m5O|XDqM7:TR?= M{j0blI1KGh? M4rLOIlv\HWlZYOgNlUvOcLiwsJCpFMvOsLiJTDhdI9xfG:|aYO= M2TGdFI2QDN3N{W1
primary MCL MYHBdI9xfG:|aYOgRZN{[Xl? MkfxNkDDvU1? NWPCZlllOjRiaB?= M2G4VYlv[3KnYYPld{B{cWewaX\pZ4FvfGy7IHHwc5B1d3Orc9Mg MXmyOVM5QDN5Mx?=
PBMCs NYjTOHE5S2WubDDWbYFjcWyrdImgRZN{[Xl? NVfITYgyOC13MDFOwG0> Mmq1NlQhcA>? NWL6fIhITE2VTx?= M{TpWYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MYCyOVEzPzh4Mh?=
PBMCs Ml;iSpVv[3Srb36gRZN{[Xl? MkXTOUDPxE1? NELGUIEyKGh? NVz0[Y9CTE2VTx?= NVvve|Jn\GWlcnXhd4V{KHSqZTDj[YxtKG2rZ4LheIlwdg>? NGPqc40zPTF{N{i2Ni=>
CFSE-CD4+ T  NX;TW3doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMlA3OjVvMTFOwG0> MnHROEBl Mk\YZoxw[2u|IIDyc4xq\mW{YYTpc44hd2ZiR2\ISE1l\XKrdnXkJGNFPCwEoGSgZ4VtdHNiYX7kJGNFOTGkK9MgZ4VtdHN? NXG2cWVqOjR4N{m5PFI>
CFSE-CD11b+ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\vNVMxNjB4MkWtNUDPxE1? NVjoRXVUQCCm NHfXc3pjdG:la4OgdJJwdGmoZYLheIlwdiCxZjDHWmhFNWSncnn2[YQhS0R2K9MgWEBk\WyuczDhcoQhS0RzMXKrxsBk\Wyucx?= NGjlZVYzPDZ5OUm4Ni=>
HMECs NGnRUIlHfW6ldHnvckBCe3OjeR?= NUXydW5[OC1zMDFOwG0> MUSyNEBucW5? NIHOOnNqdmirYnn0d{BXTUeILYP0bY12dGG2ZXSgdoVt\WG|ZTDv[kBPVw>? MoeyNlQ{Ojl3NES=
AB5 M3nrZ2Fxd3C2b4Ppd{BCe3OjeR?= MkXPNE0zNjVizszN NY\wbVd[PDhiaB?= NH3vOoVFVVOR NH;YSnFqdmS3Y3XzJIFxd3C2b4Ppdy=> Ml[xNlM{QTh7MUG=
JB7 Ml\nRZBweHSxc3nzJGF{e2G7 MlvHNE0zNjVizszN MkTkOFghcA>? MkHlSG1UVw>? NYjGbodncW6mdXPld{BieG:ydH;zbZM> M3HTNFI{Ozl6OUGx
AB5 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TrfFAuOi53IN88US=> M4n5cVQ5KGh? MY\EUXNQ MnLxbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MYiyN|M6QDlzMR?=
JB7 M3rUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW2fmMxNTJwNTFOwG0> M2nKWlQ5KGh? Mor6SG1UVw>? NUnHZnd7cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NF3QbVUzOzN7OEmxNS=>
RL NUfnRm15TnWwY4Tpc44hSXO|YYm= M4rOdFIvPS93IN88US=> MmrHNlQwPDhiaB?= M2PEdWROW09? NVH3XJFScW6mdXPld{BiKHCxdHXueEBl\WO{ZXHz[UBqdiCPTWCtPUBuWk6DIHX4dJJme3Orb36= MVOyNVkzPjl4NR?=
RL Mnu1SpVv[3Srb36gRZN{[Xl? MoG0NU8zNjVizszN MWKyOEBp MlLOSG1UVw>? Mlz1doVlfWOnczD0bIUh[WO2aY\heIlwdiCxZjDBb5Qh[W6mIIC3NHM3Uw>? M3LKVlIyQTJ4OU[1
platelet  MkLjSpVv[3Srb36gRZN{[Xl? M2LzSVHDqM7:bR?= M4XrcVUhdWmw NIHXTplqdmirYnn0d{BH[87|UlnJRU1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdg>? NHvwWYQzOTh2OE[5OC=>
platelet  MkHzSpVv[3Srb36gRZN{[Xl? MXqwMlA2NzFxMj61JO69VQ>? MoTMOUBucW5? MnHlbY5pcWKrdIOgeIhmKHOrZ37hcIlv\yCvZXPoZY5qe22|IHTve45{fHKnYX2gc4YhTmQQs2LJTWE> MUGyNVg1QDZ7NB?=
DoHH2 M3eyNmFxd3C2b4Ppd{BCe3OjeR?= NEXUeooxNzNxMUCg{txO MWm0PEBp MYfpcoR2[2W|IHPlcIwh\GWjdHigd4lodmmoaXPhcpRtgQ>? M2LRTVIxQDd3NEC4
Jeko-1  MXXBdI9xfG:|aYOgRZN{[Xl? MUKwM|MwOTBizszN MoTROFghcA>? NUPzV|dFcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MX:yNFg4PTRyOB?=
Raji  MV\BdI9xfG:|aYOgRZN{[Xl? MmPSNE8{NzFyIN88US=> M{TRZlQ5KGh? NXnPdopJcW6mdXPld{Bk\WyuIHTlZZRpKHOrZ37p[olk[W62bIm= MUCyNFg4PTRyOB?=
DHL4 M3XBUWFxd3C2b4Ppd{BCe3OjeR?= NHLEdGUxNzFxNDFOwG0> M{Py[lk3KGh? M3r0O4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NIjqVIsyQDByNk[5Oi=>
LY7 NUDkPZUxSXCxcITvd4l{KEG|c3H5 NV\OWIROOC9zL{Sg{txO Mo\xPVYhcA>? NIrjS3dqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NEDHW2gyQDByNk[5Oi=>
LY3 M{XWeWFxd3C2b4Ppd{BCe3OjeR?= NGHxT2IxNzFxNDFOwG0> MVW5OkBp MXHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnTiNVgxODZ4OU[=
DHL6 M1rTe2Fxd3C2b4Ppd{BCe3OjeR?= NVnhfJU2OC9zL{Sg{txO NVPtXndyQTZiaB?= MnvHbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHS3cWYyQDByNk[5Oi=>
LY10 M1;pR2Fxd3C2b4Ppd{BCe3OjeR?= NGD0ZnAxNzFxNDFOwG0> NEfBRnU6PiCq NH7y[pBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVjSUmNkOThyME[2PVY>
DHL10 MWHBdI9xfG:|aYOgRZN{[Xl? M1jGUVAwOS92IN88US=> M{fu[|k3KGh? NHvnZlRqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MUWxPFAxPjZ7Nh?=
Wsu-NHL M33qOWFxd3C2b4Ppd{BCe3OjeR?= M{O0PFAwOS92IN88US=> MXS5OkBp MUnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M4nJ[FE5ODB4Nkm2
LY18 MlK4RZBweHSxc3nzJGF{e2G7 NHLqXFIxNzFxNDFOwG0> M4O5c|k3KGh? MlnHbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MWSxPFAxPjZ7Nh?=
LY1 MVrBdI9xfG:|aYOgRZN{[Xl? NFu0WFAxNzFxNDFOwG0> Moq3PVYhcA>? Ml3GbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHnLdJkyQDByNk[5Oi=>
DHL8 NWXxeWtESXCxcITvd4l{KEG|c3H5 NUDpfmJwOC9zL{Sg{txO NH60RmE6PiCq NFHibW9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NFfQPY8yQDByNk[5Oi=>
DHL4 NUn6VXZrSXCxcITvd4l{KEG|c3H5 Ml7LOEDPxE1? MV25OkBp M4[weYlv\HWlZYOgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[ZMhQSCjbnSgN{wh[nW2IH7veEBk[XOyYYPlJFg> NWDxVppvOThyME[2PVY>
DHL6 NFLkWGNCeG:ydH;zbZMhSXO|YYm= NGrCXY01KM7:TR?= M{fKVlk3KGh? NGjv[4RqdmS3Y3XzJINt\WG4YXflJI9nKGOjc4Dhd4V{KDliYX7kJFMtKGK3dDDuc5Qh[2G|cHHz[UA5 NIn0RYEyQDByNk[5Oi=>
LY3 Mln3RZBweHSxc3nzJGF{e2G7 NESz[mk1KM7:TR?= NEGzSXo6PiCq MU\pcoR2[2W|IHPs[YF3[WenIH;mJINie3Cjc3XzJFkh[W6mIEOsJIJ2fCCwb4SgZ4F{eGG|ZTC4 NFrUW2syQDByNk[5Oi=>
LY7 NG\xZWtCeG:ydH;zbZMhSXO|YYm= NIi0[Wk1KM7:TR?= NE\5XWY6PiCq Mmr6bY5lfWOnczDjcIVifmGpZTDv[kBk[XOyYYPld{A6KGGwZDCzMEBjfXRibn;0JINie3Cjc3WgPC=> M334UVE5ODB4Nkm2
DHL4 NFrxZ2xHfW6ldHnvckBCe3OjeR?= MonVOEDPxE1? NXi3WWtJOTZiaB?= M4nYWolvcGmkaYTzJJRwdmmlIFLMUmshfHm{b4PpcoUheGixc4Doc5J6dGG2aX;u NFfNNJkyQDByNk[5Oi=>
LY7 NYPEWZNqTnWwY4Tpc44hSXO|YYm= MkXROEDPxE1? NHfBcnMyPiCq NH3ufIRqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> MoXzNVgxODZ4OU[=
LY3 MVrGeY5kfGmxbjDBd5NigQ>? MW[0JO69VQ>? NWHUdIFuOTZiaB?= NVnhc3hEcW6qaXLpeJMhfG:waXOgRmxPUyC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44> Mm[yNVgxODZ4OU[=
DHL6 NU[2U3JJTnWwY4Tpc44hSXO|YYm= NELxRnA1KM7:TR?= M2HHcVE3KGh? NILjUmNqdmirYnn0d{B1d26rYzDCUG5MKHS7cn;zbY5mKHCqb4PwbI9zgWyjdHnvci=> NGnjflcyQDByNk[5Oi=>
LY10 NX7nWVJUTnWwY4Tpc44hSXO|YYm= M3nNNFQh|ryP M4W1c|E3KGh? MoHPbY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NXvVV2FTOThyME[2PVY>
Wsu-NHL NUP3VIFHTnWwY4Tpc44hSXO|YYm= NF\aTVE1KM7:TR?= MonmNVYhcA>? Ml7ObY5pcWKrdIOgeI9vcWNiQlzOT{B1gXKxc3nu[UBxcG:|cHjvdplt[XSrb36= NVni[WZkOThyME[2PVY>
LY18 M1f3bGZ2dmO2aX;uJGF{e2G7 MWC0JO69VQ>? M1nFdlE3KGh? MXzpcohq[mm2czD0c45q[yCETF7LJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbh?= NXz1O5N[OThyME[2PVY>

... 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
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

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