| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R422613-1ml |
1ml |
现货  |
|
| 英文别名 | 4(3H)-Quinazolinone,2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[3H-indole-3,4'-piperidine]-1'(2H)-yl]-5,6,7,8-tetrahydro- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | RK-287107 |
| 生化机理 | RK-287107 是一种新型、强效和选择性的坦克酶抑制剂，具有抗肿瘤活性。RK-287107 在体外抑制坦克yrase-1 和坦克yrase-2 的 IC50 分别为 14.3 nM 和 10.6 nM。 |
| 储存温度 | 避光,-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 | 毒蕈碱酶抑制剂;毒蕈碱酶 2 抑制剂 |
| 产品介绍 |
RK-287107 是一种新型有效且具有选择性及抗肿瘤活性的 tankyrase 的抑制剂。RK-287107 可抑制 tankyrase-1 和 tankyrase-2，在体外实验中其IC50值为14.3 nM和10.6 nM。 Information RK-287107 RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. Targets Tankyrase-2 (Cell-free assay); Tankyrase-1 (Cell-free assay) 10.6 nM; 14.3 nM In vitro RK-287107 is a novel tankyrase-specific inhibitor that inhibits tankyrase-1 and -2. RK-287107 causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity and the target gene expression in colorectal cancer cells harboring the shortly truncated APC mutations. Consistently, RK-287107 inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells but not the APC-wild (β-catenin-independent) colorectal cancer RKO cells. In vivo Intraperitoneal or oral administration of RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice. RK-287107 suppresses the Wnt/β-catenin pathway and tumor growth of the xenografted COLO-320DM cells in vivo. Cell Research(from reference) Cell lines：COLO-320DM, HCC2998, HCT-116, DLD-1, SW403, RKO Concentrations：0.01-10 μM Incubation Time：120 h |
| ALogP | 2.731 |
|---|---|
| HBD Count | 2 |
| Rotatable Bond | 3 |
| 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 | 未知 |
|---|---|
| IIUPAC Name | 2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[2H-indole-3,4'-piperidine]-1'-yl]-5,6,7,8-tetrahydro-3H-quinazolin-4-one |
| INCHI | 1S/C22H26F2N4O2/c23-14-11-16(24)19-18(12-14)28(9-10-29)13-22(19)5-7-27(8-6-22)21-25-17-4-2-1-3-15(17)20(30)26-21/h11-12,29H,1-10,13H2,(H,25,26,30) |
| InChi Key | FZQYCOUBRJEYBC-UHFFFAOYSA-N |
| Smiles | C1CCC2=C(C1)C(=O)NC(=N2)N3CCC4(CC3)CN(C5=C4C(=CC(=C5)F)F)CCO |
| Isomeric SMILES | C1CCC2=C(C1)C(=O)NC(=N2)N3CCC4(CC3)CN(C5=C4C(=CC(=C5)F)F)CCO |
| PubChem CID | 137701512 |
| 分子量 | 416.46 |
| 敏感性 | 对光线敏感 |
|---|---|
| DMSO(mg / mL) Max Solubility | 83 |
| DMSO(mM) Max Solubility | 199.298852230706 |
| Water(mg / mL) Max Solubility | ˂1 |
| 分子量 | 416.500 g/mol |
| XLogP3 | 2.200 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 6 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 416.202 Da |
| 单同位素质量Monoisotopic Mass | 416.202 Da |
| 拓扑极表面积Topological Polar Surface Area | 68.200 Ų |
| 重原子数Heavy Atom Count | 30 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 762.000 |
| 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 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | 警告 |
| 危险声明 |
H302: 吞食有害 H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 |
首页
400-620-6333
