R406 | FLT3 | Syk | AmBeed-信号通路专用抑制剂

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R406 {[allProObj[0].p_purity_real_show]}

货号：A104426

R406是一种口服可用的竞争性Syk/FLT3抑制剂，用于ATP结合，Ki为30 nM。它在体外强效抑制Syk激酶活性，IC50为41 nM，测量时ATP浓度与其Km值相对应。R406减少免疫复合物介导的炎症，还抑制Lyn（IC50 = 63 nM）和Lck（IC50 = 37 nM）。

R406 化学结构
CAS号：841290-81-1

R406 3D分子结构
CAS号：841290-81-1

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R406 纯度/质量文件产品仅供科研

货号：A104426 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

Syk 亚型比较
FLT3 亚型比较

产品名称	Syk ↓ ↑	其他靶点	纯度
PRT062607 HCl	++++ Syk, IC50: 1 nM		99%+
R406	++ Syk, IC50: 41 nM		98%
Fostamatinib Disodium	++ Syk, IC50: 41 nM		99%+
Piceatannol	✔	PKC	98%
BAY 61-3606 2HCl	+++ Syk, Ki: 7.5 nM		99+%
Entospletinib	+++ Syk, IC50: 7.7 nM		99%+
MNS	+ Syk, IC50: 2.5 μM	p97,Src	98%
Fostamatinib	++ Syk, IC50: 41 nM		99%+
RO9021	+++ Syk, IC50: 5.6 nM		98%
TAK-659 HCl	++++ Syk, IC50: 3.2 nM	FLT3	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3 (D835Y), IC50: 6 nM FLT3, IC50: 22 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3 (D835Y), IC50: 0.4 nM FLT3, IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

R406 生物活性

靶点

FLT3
Syk

Syk, IC50:41 nM

描述

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 K of 30 nM. R406 blocks Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and Bcr-mediated activation of B lymphocytes. 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. R406 is a potent inhibitor of platelet signaling and functions initiated by FcγRIIA cross-linking by specific antibodies or by sera from HIT patients.

R406 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
AB5	0-2.5 μM	Apoptosis Assay	48 h	induces apoptosis	23398911
AB5	0-2.5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	23398911
AMO-1	1 μM	Function Assay	3 h	reduces migration	26251761
CFSE-CD11b+	0.0625-1 μM	Growth Inhibition Assay	8 d	blocks proliferation of GVHD-derived CD4+ T cells and CD11b+ cells	24679982

R406 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.95mL

1.59mL

0.80mL

15.91mL

3.18mL

1.59mL

R406 技术信息

CAS号	841290-81-1
分子式	C₂₈H₂₉FN₆O₈S
分子量	628.629

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 60 mg/mL(95.45 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 4% DMSO+4% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

AB5	0-2.5 μM	Apoptosis Assay	48 h	induces apoptosis	23398911
AB5	0-2.5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	23398911
AMO-1	1 μM	Function Assay	3 h	reduces migration	26251761
CFSE-CD11b+	0.0625-1 μM	Growth Inhibition Assay	8 d	blocks proliferation of GVHD-derived CD4+ T cells and CD11b+ cells	24679982
CFSE-CD4+ T	0.0625-1 μM	Growth Inhibition Assay	4 d	blocks proliferation of GVHD-derived CD4+ T cells and CD11b+ cells	24679982
DHL10	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
DHL4	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
DHL4	4 μM	Apoptosis Assay	96 h	induces cleavage of caspases 9 and 3, but not caspase 8	18006696
DHL4	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696
DHL6	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
DHL6	4 μM	Apoptosis Assay	96 h	induces cleavage of caspases 9 and 3, but not caspase 8	18006696
DHL6	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696
DHL8	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
DoHH2	0/3/10 μM	Apoptosis Assay	48 h	induces cell death significantly	20875408
HMECs	0-10 μM	Function Assay	20 min	inhibits VEGF-stimulated release of NO	24329544
JB7	0-2.5 μM	Apoptosis Assay	48 h	induces apoptosis	23398911
JB7	0-2.5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	23398911
Jeko-1		Growth Inhibition Assay	48 h	IC50=5.06826 μM	25835755
Jeko-1	5 μM	Apoptosis Assay	24 h	induces 25.1 ± 3.2 % apoptosis	25835755
Jeko-1	0/3/10 μM	Apoptosis Assay	48 h	induces cell death significantly	20875408
LY1	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
LY10	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
LY10	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696
LY18	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
LY18	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696
LY3	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
LY3	4 μM	Apoptosis Assay	96 h	induces cleavage of caspases 9 and 3, but not caspase 8	18006696
LY3	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696
LY7	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
LY7	4 μM	Apoptosis Assay	96 h	induces cleavage of caspases 9 and 3, but not caspase 8	18006696
LY7	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696
Mino		Growth Inhibition Assay	48 h	IC50=5.70854 μM	25835755
PBMCs	0-50 μM	Cell Viability Assay	24 h	inhibits cell viability dose dependently	25127862
PBMCs	5 μM	Function Assay	1 h	decreases the cell migration	25127862
platelet	1 μm	Function Assay	5 min	inhibits FcγRIIA-mediated platelet aggregation	21848694
platelet	0.05/1/2.5 μM	Function Assay	5 min	inhibits the signaling mechanisms downstream of FcγRIIA	21848694
primary MCL	2 µM	Apoptosis Assay	24 h	increases significantly apoptosis	25388373
Raji	0/3/10 μM	Apoptosis Assay	48 h	induces cell death significantly	20875408
RL	2.5/5 μM	Function Assay	24/48 h	induces a potent decrease in MMP-9 mRNA expression	21926965
RL	1/2.5 μM	Function Assay	24 h	reduces the activation of Akt and p70S6K	21926965
U266	1 μM	Function Assay	3 h	reduces migration	26251761
Wsu-NHL	0/1/4 μM	Apoptosis Assay	96 h	induces apoptosis dose dependently	18006696
Wsu-NHL	4 μM	Function Assay	16 h	inhibits tonic BLNK tyrosine phosphorylation	18006696

R406 {[allProObj[0].p_purity_real_show]}

R406 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

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R406 生物活性

R406 细胞研究

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R406 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

R406 质控信息

R406 生物活性

R406 细胞研究

R406 实验方案

R406 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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R406 纯度/质量文件产品仅供科研