CH7057288
规格
| Cas Number | 2095616-82-1 |
| 规格或纯度 | Moligand™, ≥99% |
| 级别 | Moligand™ |
| 纯度 | ≥99% |
| 包装 | 100mg 或 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 | 神经营养受体酪氨酸激酶 1 抑制剂；神经营养受体酪氨酸激酶 2 抑制剂；神经营养受体酪氨酸激酶 3 抑制剂 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (175.54 mM); Water: Insoluble; Ethanol: Insoluble; |
| 简短描述 | TrkA 选择性抑制剂 |
| 英文简短描述 | TrkA Selective Inhibitors |
| 过滤标签 | neurotrophic receptor tyrosine kinase 1 Inhibitor,neurotrophic receptor tyrosine kinase 2 Inhibitor,neurotrophic receptor tyrosine kinase 3 Inhibitor,Trk Receptor,Protein Tyrosine Kinase/RTK,神经元信号传导 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | CH7057288 是一种强效的选择性 TRK 抑制剂，对 TRKA、TRKB 和 TRKC 的 IC50 值分别为 1.1 nM、7.8 nM 和 5.1 nM。 |
| 描述 |
CH7057288是一种有效的、选择性TRK抑制剂，对TRKA、TRKB和TRKC的IC50值分别为1.1 nM, 7.8 nM和5.1 nM。 |
| 英文描述 |
Information CH7057288 is a potent and selectiveTRKinhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively. Targets TrkA (Cell-free assay); TrkC (Cell-free assay); TrkB (Cell-free assay) 1.1 nM; 5.1 nM; 7.8 nM In vitro CH7057288 shows selective inhibitory activity against TRKA, TRKB, and TRKC in cell-free kinase assays and suppresses proliferation of TRK fusion-positive cell lines, but not that of TRK-negative cell lines. CH7057288 suppresses mitogen-activated protein kinase (MAPK) and E2F pathways as downstream signaling of TRK fusion. In vivo Strong in vivo tumor growth inhibition is observed in subcutaneously implanted xenograft tumor models of TRK fusion-positive cells. Furthermore, in an intracranial implantation model mimicking brain metastasis, CH7057288 significantly induces tumor regression and improves event-free survival. CH7057288 induces potent tumor growth inhibition against all three models, with remarkable tumor regression in CUTO-3 and MO-91. CH7057288 exhibits dose-dependent exposure. Because of relatively short terminal half-life (3 to 5 hours), the plasma concentration 24 hours after dose dropped to approximately a few tenths to a hundredth of Tmax. Cell Research(from reference) Cell lines：The NSCLC cell line CUTO-3, CRC cell line KM12-Luc, and acute myeloid leukemia cell line MO-91 harbor MPRIP-NTRK1, TPM3-NTRK1, and ETV6-NTRK3, respectively Concentrations：0.01, 0.1 and 1 μM Incubation Time：2 h |