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Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 {[allProObj[0].p_purity_real_show]}

货号:A158498 同义名: R788 disodium hexahydrate; Tavalisse

Fostamatinib disodium hexahydrate是一种 Syk 抑制剂,IC50 为 41 nM,同时是代谢产物 R406 的前药,具有免疫调节活性。

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 化学结构 CAS号:914295-16-2
Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 化学结构
CAS号:914295-16-2
Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 3D分子结构
CAS号:914295-16-2
Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 化学结构 CAS号:914295-16-2
Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 3D分子结构 CAS号:914295-16-2
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Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 纯度/质量文件 产品仅供科研

货号:A158498 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 生物活性

描述 Fostamatinib (R788) disodium hexahydrate serves as the oral prodrug of the active compound R406 [1].

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 细胞实验

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDM) 500 nmol/L 24 hours To investigate the effect of Fostamatinib on macrophage polarization. Results showed that Fostamatinib prevented IL4-induced expression of immunosuppressive genes and downregulated the expression of these genes in macrophages cocultured with KPC1245 tumor cells. Cancer Res. 2023 Aug 15;83(16):2675-2689.

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice (C57BL/6) Orthotopic pancreatic ductal adenocarcinoma (PDAC) model Intraperitoneal injection 50 mg/kg Five times per week, continuous treatment To evaluate the effect of Fostamatinib alone or in combination with gemcitabine on PDAC growth and metastasis. Results showed that Fostamatinib significantly reduced tumor growth and metastasis and remodeled the tumor immune microenvironment, enhancing CD8+ T cell responses. Cancer Res. 2023 Aug 15;83(16):2675-2689.
NOD.SCID mice Xenogeneic model of EBV+ B-cell lymphoma Oral fostamatinib-containing chow Continuous administration Syk inhibition did not significantly affect solid tumor growth but resulted in tumor growth in adjacent inguinal lymph nodes Am J Transplant. 2013 Apr;13(4):883-890.
Mice Wild-type neonatal mice Oral 40 mg/kg body weight Every 6 hours for 8 days To evaluate the effect of SYK inhibitor fostamatinib on the lymphatic system, results showed no detectable entry of blood into the thoracic duct J Clin Invest. 2014 Jan;124(1):273-84
C57BL/6J mice Ischemia/reperfusion (I/R)-induced acute lung injury model Oral 3 g/kg Once daily for 10 days To evaluate the effect of Fostamatinib (R788) on MUC1 levels in a model of acute lung injury. Results showed that Fostamatinib significantly reduced MUC1 abundance in lung epithelial cells. Cell Rep Med. 2020 Oct 29;1(8):100137.
Apoe-/- mice High cholesterol diet-induced atherosclerosis model Dietary administration 0.3% (w/w) Continuous for 8 or 20 weeks Evaluate the effect of Fostamatinib on early and late-stage atherosclerosis. Results showed Fostamatinib significantly reduced plaque size and macrophage accumulation in early lesions but had limited effect in late-stage lesions. Basic Res Cardiol. 2016 Mar;111(2):20.
NOD/SCID gamma mice Subcutaneous xenograft model Intraperitoneal injection 40 mg/kg and 80 mg/kg Daily administration for 33 days To evaluate the inhibitory effect of Fostamatinib on xenograft tumor growth. Cell Mol Gastroenterol Hepatol. 2018 Jan 31;5(4):569-590

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 参考文献

[1]Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273.

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.37mL

0.27mL

0.14mL

6.83mL

1.37mL

0.68mL

13.65mL

2.73mL

1.37mL

Fostamatinib disodium hexahydrate/福他替尼二钠盐六水合物 技术信息

CAS号914295-16-2
分子式C23H36FN6Na2O15P
分子量 732.51
SMILES Code O=C1N(COP([O-])([O-])=O)C2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC1(C)C.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+].[Na+]
MDL No. MFCD19443649
别名 R788 disodium hexahydrate; Tavalisse; Tamatinib Fosdium hexahydrate
运输蓝冰
InChI Key ZQGJCHHKJNSPMS-UHFFFAOYSA-L
Pubchem ID 24828759
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

DMSO: 25 mg/mL(34.13 mM),配合低频超声助溶,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

H2O: 2 mg/mL(2.73 mM),配合低频超声,并水浴加热至45℃助溶

配制的工作液建议现用现配,短期内尽快用完。 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
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