| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B425289-1ml |
1ml |
现货  |
|
| 英文别名 | MS-28520 | 2-(7-(3,4-Dimethoxyphenyl)imidazo(1,2-c)pyrimidin-5-ylamino)nicotinamide dihydrochloride | BAY 61-3606 (dihydrochloride) | YAB90357 | AKOS027276142 | HY-14985 | DTXSID20215179 | 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-p |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | BAY-61-3606 |
| 生化机理 | BAY-61-3606 是一种强效的 Syk 激酶选择性抑制剂（Ki = 7.5 nM）。BAY-61-3606 可诱导细胞周期停滞和细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
BAY 61-3606 dihydrochloride 是一种口服有效的，ATP 竞争性的，可逆的选择性 Syk 抑制剂，Ki 为 7.5 nM，IC50 为 10 nM。BAY 61-3606 dihydrochloride 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 dihydrochloride 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 dihydrochloride 作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。 Information BAY-61-3606 BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis . Targets Syk (Cell-free assay) 7.5 nM(Ki) In vitro BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM. In vivo After 20 days of drug administration, the volume of the xenografted tumor was significantly (P <0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination. Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats. Cell Research(from reference) Cell lines：MCF-7 cells Concentrations：2.5 μM or 5 μM Incubation Time：12 h or 24 h |
| ALogP | 3.082 |
|---|---|
| HBD Count | 2 |
| Rotatable Bond | 6 |
| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| 活性类型 | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| 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-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide;dihydrochloride |
| INCHI | InChI=1S/C20H18N6O3.2ClH/c1-28-15-6-5-12(10-16(15)29-2)14-11-17-22-8-9-26(17)20(24-14)25-19-13(18(21)27)4-3-7-23-19;;/h3-11H,1-2H3,(H2,21,27)(H,23,24,25);2*1H |
| InChi Key | SPMFEULFGGPQLN-UHFFFAOYSA-N |
| Canonical SMILES | COC1=C(C=C(C=C1)C2=CC3=NC=CN3C(=N2)NC4=C(C=CC=N4)C(=O)N)OC.Cl.Cl |
| Isomeric SMILES | COC1=C(C=C(C=C1)C2=CC3=NC=CN3C(=N2)NC4=C(C=CC=N4)C(=O)N)OC.Cl.Cl |
| PubChem CID | 11784504 |
| 分子量 | 463.32 |
| DMSO(mg / mL) Max Solubility | 14 |
|---|---|
| DMSO(mM) Max Solubility | 30.21669688 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 463.300 g/mol |
| XLogP3 | |
| 氢键供体数Hydrogen Bond Donor Count | 4 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 462.097 Da |
| 单同位素质量Monoisotopic Mass | 462.097 Da |
| 拓扑极表面积Topological Polar Surface Area | 117.000 Ų |
| 重原子数Heavy Atom Count | 31 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 566.000 |
| 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 | 3 |
| concentration | 9.0-11.0（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to structure |
首页
400-620-6333
