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抑制剂/激动剂
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蛋白质酪氨酸激酶 肿瘤发展和微环境演变
/ Syk / R406 free base

R406 free base {[allProObj[0].p_purity_real_show]}

货号：A233735 同义名： R406; free base

R406 free base是一种口服有效且竞争性Syk/FLT3抑制剂，其对ATP结合的Ki为30 nM，有效抑制体外Syk激酶活性，IC50为41 nM，在与其Km值相对应的ATP浓度下测量。它减少了免疫复合物介导的炎症，还抑制Lyn（IC50 = 63 nM）和Lck（IC50 = 37 nM）。

R406 free base 化学结构 CAS号：841290-80-0
R406 free base 化学结构
CAS号：841290-80-0
R406 free base 3D分子结构
CAS号：841290-80-0
R406 free base 化学结构 CAS号：841290-80-0
R406 free base 3D分子结构 CAS号：841290-80-0
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R406 free base 纯度/质量文件 产品仅供科研

货号：A233735 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

R406 free base 生物活性

描述 R406 is a potent Syk inhibitor with IC50 of 41 nM that strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.

R406 free base 细胞实验

Cell Line
Concentration Treated Time Description References
SKOV3TR 2.5 µM Enhanced paclitaxel cytotoxicity Cancer Cell. 2015 Jul 13;28(1):82-96.
MPSC1 2.5 µM Inhibited cell proliferation Cancer Cell. 2015 Jul 13;28(1):82-96.
MPSC1TR 2.5 µM Enhanced paclitaxel cytotoxicity Cancer Cell. 2015 Jul 13;28(1):82-96.
U87 10 μM 48 h R406 showed weak inhibitory effect on U87 cells, with an IC50 greater than 1 mM. Cell Death Dis. 2019 May 1;10(5):358.
C17.2 10 μM 48 h R406 showed no significant toxicity to C17.2 cells. Cell Death Dis. 2019 May 1;10(5):358.
CD19-selected spleen lymphocytes 2.5 μM 48 h R406 inhibits the B-cell receptor signaling pathway, leading to decreased expression of Foxm1 and Ccl3, and increased expression of p53. Leukemia. 2015 Jun;29(6):1350-9.
CH12 cells 1.85 μM 18 h R406 inhibits BCR signaling, reducing phosphorylated proteins including pBTK, but not affecting pSYK. Immunity. 2023 Oct 10;56(10):2373-2387.e8.
CH12 cells 1.85 μM 18 h R406 inhibits BCR signaling, enhancing CH12-M and CH12-A sensitivity to FasL vesicles, leading to increased cell death. Immunity. 2023 Oct 10;56(10):2373-2387.e8.
BV2 cells 1 mM 2 h To suppress SYK to mitigate neuroinflammation Neural Regen Res. 2024 Jun 1;19(6):1375-1384.
microglia 1 mM 24 h Inhibit SYK to detect its effect on microglial inflammatory response Cell Death Dis. 2019 Jul 19;10(8):555.
SKOV3 2.5 µM 48 h Inhibited SYK autophosphorylation, reduced cell proliferation Cancer Cell. 2015 Jul 13;28(1):82-96.
chronic lymphocytic leukemia cells 100 μM 1 h To investigate the effect of R406 on chronic lymphocytic leukemia cells, results showed that R406 inhibited the anti-apoptotic effect mediated by sLAG3 Haematologica. 2017 May;102(5):874-882.
B1-8 splenic B cells 5 μM 60 min To test the effect of Syk inhibitor R406 on B cell activation, results showed that R406 completely blocked the dissociation of BCR oligomers. Elife. 2014 Jun 24;3:e02069.
TKO-M cells 5 μM 60 min To test the effect of Syk inhibitor R406 on BCR oligomer dissociation, results showed that R406 increased the antigen dose required for BCR oligomer dissociation. Elife. 2014 Jun 24;3:e02069.
GSC-1 1 μM 48 h R406 significantly inhibited the proliferation of GSC-1 cells, with an IC50 of 0.75 μM. Cell Death Dis. 2019 May 1;10(5):358.
GSC-2 1 μM 48 h R406 significantly inhibited the proliferation of GSC-2 cells, with an IC50 of 0.89 μM. Cell Death Dis. 2019 May 1;10(5):358.
U251 10 μM 48 h R406 showed weak inhibitory effect on U251 cells, with an IC50 greater than 1 mM. Cell Death Dis. 2019 May 1;10(5):358.

R406 free base 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice K14-HPV16 transgenic mice Orally 2.0 g/kg Starting at 1 month of age and continuing for a total of 12 weeks R406, by inhibiting Syk kinase activity, prevented the progression from hyperplasia to dysplasia/carcinoma in situ in K14-HPV16 mice. Cancer Cell. 2014 Jun 16;25(6):809-821
Mice MPTP-induced Parkinson's disease model Intraperitoneal injection 5 mg/kg Once daily for five consecutive days To suppress SYK to mitigate neuroinflammation Neural Regen Res. 2024 Jun 1;19(6):1375-1384.
Mice MCAO model Intraperitoneal injection 5 mg/kg Once daily for 3 consecutive days Inhibit SYK to detect its effect on post-ischemic inflammatory response Cell Death Dis. 2019 Jul 19;10(8):555.
Mice SKOV3c.2 subcutaneous tumor model Orally 6.5 mg/kg Three-days on/three-days off cycles for four cycles Combination with paclitaxel significantly reduced tumor weight Cancer Cell. 2015 Jul 13;28(1):82-96.
BALB/c-nu/nu mice Subcutaneous tumor model Intraperitoneal injection 20 mg/kg Once daily until tumor volume reached 1000 mm³ R406 significantly delayed subcutaneous tumor growth and synergized with TMZ to inhibit tumor. Cell Death Dis. 2019 May 1;10(5):358.

R406 free base 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01725230 Rheumatoid Arthritis Phase 1 Completed - United States, Kansas ... 展开 >> Research Site Overland Park, Kansas, United States 收起 <<
NCT01208155 Bioavailability ... 展开 >> Pharmacokinetics 收起 << Phase 1 Completed - United States, Kansas ... 展开 >> Research Site Overland Park, Kansas, United States 收起 <<
NCT01245790 Rheumatoid Arthritis ... 展开 >> Renal Impairment 收起 << Phase 1 Completed - United States, Florida ... 展开 >> Research Site Orlando, Florida, United States 收起 <<

R406 free base 参考文献

[1]Chen L, Monti S, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood. 2008 Feb 15;111(4):2230-7.

[2]Braselmann S, Taylor V, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

R406 free base 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.63mL

2.13mL

1.06mL

21.26mL

4.25mL

2.13mL

R406 free base 技术信息

CAS号841290-80-0
分子式C22H23FN6O5
分子量 470.45
SMILES Code O=C1NC2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC1(C)C
MDL No. MFCD09970820
别名 R406; free base
运输蓝冰
InChI Key NHHQJBCNYHBUSI-UHFFFAOYSA-N
Pubchem ID 11213558
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 25 mg/mL(53.14 mM)，配合低频超声，并水浴加热至45℃助溶，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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: R406 free base | R406;free base | Syk | AmBeed-信号通路专用抑制剂 | R406 free base 纯度/质量文件 | R406 free base 亚型比较 | R406 free base 生物活性 | R406 free base 临床数据 | R406 free base 参考文献 | R406 free base 实验方案 | R406 free base 技术信息

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