| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| F408264-1ml |
1ml |
现货  |
|
| 别名 | 福他替尼 (R788) |
|---|---|
| 英文别名 | (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2,3-dihydropyrido[3,2-b][1,4]oxazin-4-yl)methyl dihydrogen phosphate |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Fostamatinib (R788) |
| 生化机理 | 福斯他替尼（R788）是活性代谢物 R406 的原药，是一种 Syk 抑制剂，IC50 为 41 nM，能强烈抑制 Syk，但不能抑制 Lyn，对 Flt3 的抑制作用弱 5 倍。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 酪氨酸蛋白激酶 SYK 抑制剂 |
| 产品介绍 |
Fostamatinib (R788)是活性代谢产物R406的前体药物，是一种Syk抑制剂，IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果低5倍。Phase 3。An inhibitor to spleenic kinase-mediated IgG Fc receptor signaling Information Fostamatinib (R788) Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3. R788 is a prodrug of the spleen tyrosine kinase (Syk) inhibitor R406. R788 is a competitive inhibitor for ATP binding with a Ki of 30 nM. R788 dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM. R788 also inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. Inhibition of Syk by R788 results in inhibition of all phosphorylation events downstream of Syk signaling. Next to FcϵRI signaling in CHMC, R788 most potently inhibits the signaling of IL-4 and IL-2 receptors. R788 specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes. R788 induces apoptosis of the majority of examined DLBCL cell lines. In R788-sensitive DLBCL cell lines, R788 specifically inhibits both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYK-dependent phosphorylation of the B-cell linker protein [BLNK]). In vivo Oral administration of R788 to mice reduces immune complex-mediated inflammation in a reverse-passive Arthus reaction and two antibody-induced arthritis models. In another study, R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolongs survival of the treated animals. R788 demonstrates a significant reduction in major inflammatory mediators such as TNFalpha, IL-1, IL-6 and IL-18, leading to reduced inflammation and bone degradation in models of rheumatoid arthritis. cell lines：HEY and OVCA 433 Concentrations：0 μM -100 μM Incubation Time：30 minutes Powder Purity:≥99% |
| ALogP | 3.458 |
|---|---|
| hba_count | 9 |
| HBD Count | 2 |
| Rotatable Bond | 10 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=C(OC)C(=CC(=C1)NC2=NC=C(F)C(=N2)NC3=CC=C4OC(C)(C)C(=O)N(CO[P](O)(O)=O)C4=N3)OC |
| 分子量 | 580.46 |
| Reaxy-Rn | 12237902 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12237902&ln= |
| DMSO(mg / mL) Max Solubility | 116 |
|---|---|
| DMSO(mM) Max Solubility | 199.84 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 12237902 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12237902&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
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