RK-287107
规格
| Cas Number | 2171386-10-8 |
| 规格或纯度 | Moligand™, ≥98% |
| 级别 | Moligand™ |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 5mg 或 25mg 或 2mg |
产品信息
| 品牌 | 阿拉丁 |
| Action Type | 抑制剂 |
| Mechanism Of Action | 毒蕈碱酶抑制剂;毒蕈碱酶 2 抑制剂 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 83 mg/mL (199.29 mM); Water: Insoluble; Ethanol: Insoluble; |
| 简短描述 | PARP抑制剂 |
| 英文简短描述 | PARP Inhibitors |
| 过滤标签 | 表观遗传学,tankyrase Inhibitor,tankyrase 2 Inhibitor,PARP,Cell Cycle/DNA Damage |
| 储存温度 | 避光,-20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | 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。 |
| 描述 |
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。 |
| 英文描述 |
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 |