| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L421370-1ml |
1ml |
现货  |
|
| 英文别名 | N-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-3-fluoro-phenyl]-4-ethoxy-1-(4-fluoro-2-methyl-phenyl)pyrazole-3-carboxamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | LDC1267 |
| 生化机理 | LDC1267 是一种高选择性 TAM 激酶抑制剂，对 Mer、Tyro3 和 Axl 的 IC50 分别小于 5 nM、8 nM 和 29 nM。对 Met、Aurora B、Lck、Src 和 CDK8 的活性较低。 |
| 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 | AXL 受体酪氨酸激酶抑制剂；MER 原癌基因酪氨酸激酶抑制剂；TYRO3 蛋白酪氨酸激酶抑制剂 |
| 产品介绍 |
Information LDC1267 LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8. Targets Mer (Cell-free assay); Tyro3 (Cell-free assay); Axl (Cell-free assay) <5 nM; 8 nM; 29 nM In vitro LDC1267 moderately affects cell proliferation in 11 of 95 different cell lines with IC50 of >5μM. In NKG2D-activated NK cells, LDC1267 abolishes the inhibitory effects of Gas6 stimulation. In vivo In B16F10 melanoma-bearing mice, LDC1267 (20 mg/kg, i.p.) efficiently enhances anti-metastatic NK cell activity, and rejects tumor metastases without serious cytotoxicity. Cell Research(from reference) Cell lines：A panel of 93 cancer cell lines and two primary cells (x axis, IMR90 and human peripheral blood mononuclear cells) Concentrations：~30 μM Incubation Time：72 hours |
| ALogP | 6.213 |
|---|---|
| hba_count | 7 |
| HBD Count | 1 |
| Rotatable Bond | 9 |
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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 | N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)pyrazole-3-carboxamide |
| INCHI | InChI=1S/C30H26F2N4O5/c1-5-40-28-16-36(23-8-6-18(31)12-17(23)2)35-29(28)30(37)34-19-7-9-25(21(32)13-19)41-24-10-11-33-22-15-27(39-4)26(38-3)14-20(22)24/h6-16H,5H2,1-4H3,(H,34,37) |
| InChi Key | ISPBCAXOSOLFME-UHFFFAOYSA-N |
| Canonical SMILES | CCOC1=CN(N=C1C(=O)NC2=CC(=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)F)C5=C(C=C(C=C5)F)C |
| Isomeric SMILES | CCOC1=CN(N=C1C(=O)NC2=CC(=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)F)C5=C(C=C(C=C5)F)C |
| 分子量 | 560.55 |
| Reaxy-Rn | 22371579 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22371579&ln= |
| DMSO(mg / mL) Max Solubility | 100 |
|---|---|
| DMSO(mM) Max Solubility | 178.396218 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 560.500 g/mol |
| XLogP3 | 5.700 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 9 |
| 可旋转键计数Rotatable Bond Count | 9 |
| 精确质量Exact Mass | 560.187 Da |
| 单同位素质量Monoisotopic Mass | 560.187 Da |
| 拓扑极表面积Topological Polar Surface Area | 96.700 Ų |
| 重原子数Heavy Atom Count | 41 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 860.000 |
| 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 | 22371579 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22371579&ln= |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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