计算溶液所需的质量、体积或浓度。
This is a demo store. No orders will be fulfilled.
| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C127975-5mg |
5mg |
现货 ![]() |
| |
| C127975-10mg |
10mg |
现货 ![]() |
| |
| C127975-50mg |
50mg |
期货 ![]() |
|
| 英文别名 | PDSP2_000002 | W-204393 | NSC761193 | NSC-761193 | DB15408 | HY-50855 | HMS3244M13 | NCGC00263192-02 | AC-28426 | Q27076934 | silmitasertibum | BENZO(C)-2,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID, 5-((3-CHLOROPHENYL)AMINO)- | J-516169 | CX-4945,CAS:1009820-21-6 |
|---|---|
| 规格或纯度 | Moligand™, ≥98% |
| 英文名称 | CX-4945 (Silmitasertib) |
| 生化机理 | CX-4945(Silmitasertib)是一种 ATP 竞争性 CK2 蛋白激酶抑制剂,对重组人 CK2α 的 Ki 和 IC50 分别为 0.38 和 1 nM。CX-4945 在多种癌细胞系中具有广谱抗增殖活性。CX-4945 对癌细胞的抗增殖活性与 CK2α 催化亚基的表达水平相关。CX-4945对PI3K/Akt信号转导的抑制作用通过Akt在CK2特异性S129位点以及典型的S473和T308调节位点上的去磷酸化得到证实。CX-4945 可抑制 Akt 信号转导并抑制 HUVEC 细胞的增殖。CX-4945 可导致细胞周期停滞,并选择性地诱导某些癌细胞凋亡。在血管生成模型中,CX-4945 可抑制人脐静脉内皮细胞迁移、管形成,并阻断癌细胞中 CK2 依赖性缺氧诱导因子 1 alpha(HIF-1α)的转录。总之,CX-4945 在体外和体内都能抑制促血管生成的 CK2 信号传导。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 酪蛋白激酶 IIα 抑制剂 |
| 产品介绍 |
CX-4945 (Silmitasertib)是有效的,选择性CK2(casein kinase 2)抑制剂,无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。An ATP-competitive CK2 protein kinase inhibitor. CX-4945 (Silmitasertib) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). |
| 纯度 | ≥98% |
| ALogP | 4.4 |
|---|
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | 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 |
|---|---|
| IIUPAC Name | 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid |
| INCHI | 1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25) |
| InChi Key | MUOKSQABCJCOPU-UHFFFAOYSA-N |
| Smiles | C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4 |
| Isomeric SMILES | C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4 |
| 分子量 | 349.77 |
| Reaxy-Rn | 13112605 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13112605&ln= |
| 溶解性 | Soluble in water (<1.2 mg/ml), DMSO (≥65 mg/ml), and ethanol (<1.2 mg/ml). |
|---|---|
| 分子量 | 349.800 g/mol |
| XLogP3 | 4.400 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 349.062 Da |
| 单同位素质量Monoisotopic Mass | 349.062 Da |
| 拓扑极表面积Topological Polar Surface Area | 75.100 Ų |
| 重原子数Heavy Atom Count | 25 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 491.000 |
| 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 |
通过匹配包装上的批号来查找并下载产品的 COA,每批产品都进行了严格的验证,您可放心使用!
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | C127975 |
| 1. Siddiqui-Jain A, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C et al.. (2010) CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy.. Cancer Res, 70 (24): (10288-98). [PMID:21159648] |
| 2. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E et al.. (2011) Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.. J Med Chem, 54 (2): (635-54). [PMID:21174434] |
| 3. Battistutta R, Cozza G, Pierre F, Papinutto E, Lolli G, Sarno S, O'Brien SE, Siddiqui-Jain A, Haddach M, Anderes K et al.. (2011) Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.. Biochemistry, 50 (39): (8478-88). [PMID:21870818] |
| 4. Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL et al.. (2020) A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.. Nature, 583 (7816): (459-468). [PMID:32353859] |