|6-[[5-氟-2-[(3,4,5-三甲氧基苯基)氨基]-4-嘧啶基]氨基]-2,2-二甲基-2H-吡啶并[3,2-b]-1,4-噁嗪-3(4H)-酮苯磺酸盐|CsnPharm

CAS No.: 841290-81-1

6-((5-Fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one benzenesulfonate Catalog No. CSN16942

Synonyms: Tamatinib Benzenesulfonate;Tamatinib,

R406 benzenesulfonate is a selective inhibitor of Syk with IC50 of 41 nM.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Syk

IC50:41nM
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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5908 mL
- 7.9538 mL
- 15.9076 mL
- 5 mM
- 0.3182 mL
- 1.5908 mL
- 3.1815 mL
- 10 mM
- 0.1591 mL
- 0.7954 mL
- 1.5908 mL

技术信息

CAS号

841290-81-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H29FN6O8S

运输

蓝冰

分子量

628.63

别名

Tamatinib Benzenesulfonate;Tamatinib,

溶解度

DMSO	25.0 mg/mL (39.8 mM) warming
Water	insoluble

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

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

6-((5-Fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one benzenesulfonate Catalog No. CSN16942

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