| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A421669-1ml |
1ml |
现货  |
|
| 英文别名 | MS-26988 | 2-(4-((5-((2,6-difluoro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)ethan-1-ol | BA166836 | 2-[4-({5-[(2,6-difluoro-3,5-dimethoxybenzyl)oxy]pyrimidin-2-yl}amino)-1H-pyrazol-1-yl]ethanol | EX-A2488 | AKOS032946247 | ASP 5878 [W |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | ASP5878 |
| 生化机理 | ASP5878 是一种新型的表皮生长因子受体选择性抑制剂，对重组表皮生长因子受体 1、2、3 和 4 的 IC50 值分别为 0.47、0.60、0.74 和 3.5 nmol/L。 |
| 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 | 成纤维细胞生长因子受体 3 抑制剂 |
| 产品介绍 |
ASP5878是新型的FGFR选择性抑制剂，对重组FGFR1、FGFR2、FGFR3和FGFR4的IC50分别为0.47, 0.60, 0.74和3.5 nM。 Information ASP5878 is a novelFGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively. Targets FGFR1 (Cell-free assay); FGFR2 (Cell-free assay); FGFR3 (Cell-free assay); FGFR4 (Cell-free assay) 0.47 nM; 0.6 nM; 0.74 nM; 3.5 nM In vitro ASP5878 inhibits the cell proliferation of HCC cell lines expressing FGF19. ASP5878 inhibits FGFR4 phosphorylation and its treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation in Hep3B2.1-7 cells. In vivo Oral administration of ASP5878 at 3 mg/kg induces sustained tumor regression in a subcutaneous xenograft mouse model using Hep3B2.1-7. In HuH-7, an orthotopic xenograft mouse model, ASP5878 induces complete tumor regression and dramatically extended the survival of the mice. Cell Research(from reference) Cell lines：Hep3B2.1-7 cells Concentrations：0-1000 nM Incubation Time：2 h |
| IC50 | FGFR1, IC50: 0.47 nM |
|---|---|
| ALogP | 2.178 |
| hba_count | 6 |
| HBD Count | 2 |
| Rotatable Bond | 9 |
| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | 2-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]pyrazol-1-yl]ethanol |
| INCHI | InChI=1S/C18H19F2N5O4/c1-27-14-5-15(28-2)17(20)13(16(14)19)10-29-12-7-21-18(22-8-12)24-11-6-23-25(9-11)3-4-26/h5-9,26H,3-4,10H2,1-2H3,(H,21,22,24) |
| InChi Key | VDZZYOJYLLNBTD-UHFFFAOYSA-N |
| Canonical SMILES | COC1=CC(=C(C(=C1F)COC2=CN=C(N=C2)NC3=CN(N=C3)CCO)F)OC |
| Isomeric SMILES | COC1=CC(=C(C(=C1F)COC2=CN=C(N=C2)NC3=CN(N=C3)CCO)F)OC |
| 分子量 | 407.37 |
| Reaxy-Rn | 26815998 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26815998&ln= |
| DMSO(mg / mL) Max Solubility | 81 |
|---|---|
| DMSO(mM) Max Solubility | 198.836438618455 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 407.400 g/mol |
| XLogP3 | 1.200 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 10 |
| 可旋转键计数Rotatable Bond Count | 9 |
| 精确质量Exact Mass | 407.141 Da |
| 单同位素质量Monoisotopic Mass | 407.141 Da |
| 拓扑极表面积Topological Polar Surface Area | 104.000 Ų |
| 重原子数Heavy Atom Count | 29 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 473.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| Reaxy-Rn | 26815998 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26815998&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless to light yellow liquid) | Pass |
| Record the entire process by video | Conform |
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