TP-0903
| 中文名称 | TP-0903 |
|---|---|
| 中文同义词 | 2-[[5-氯-2-[[4-[(4-甲基-1-哌嗪基)甲基]苯基]氨基]-4-嘧啶基]氨基]-N,N-二甲基苯磺酰胺;AXL受体酪氨酸激酶抑制剂(TP-0903);化合物TP0903;杜贝马丁尼(TP-0903) |
| 英文名称 | TP0903 |
| 英文同义词 | TP0903;TP-0903;2-[[5-Chloro-2-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-4-pyrimidinyl]amino]-N,N-dimethylbenzenesulfonamide;CS-1642;2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide;TP 0903;TP0903;Dubermatinib;Benzenesulfonamide, 2-[[5-chloro-2-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-4-pyrimidinyl]amino]-N,N-dimethyl- |
| CAS号 | 1341200-45-0 |
| 分子式 | C24H30ClN7O2S |
| 分子量 | 516.06 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;小分子抑制剂;细胞生物学试剂;Inhibitors;api |
| Mol文件 | 1341200-45-0.mol |
| 结构式 |  |
TP-0903 性质
| 熔点 | >198°C (dec.) |
|---|---|
| 沸点 | 664.7±65.0 °C(Predicted) |
| 密度 | 1.347±0.06 g/cm3(Predicted) |
| 储存条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| 溶解度 | 可溶于氯仿（少许）、甲醇（少许） |
| 酸度系数(pKa) | 7.60±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 灰白色至浅黄色 |
TP-0903 是一种有效的选择性 AXL 抑制剂，IC50 为 27 nM。TP-0903 可非常有效地诱导凋亡。
Dubermatinib is a potent and selective AXL inhibitor. TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges. Combination of TP-0903 with BTK inhibitors augments CLL B-cell apoptosis AXL overexpression is a reoccurring theme observed in multiple tumor types that have acquired resistance to various agents. Treatment of cancer cells with TP-0903 reverses the mesenchymal phenotype in multiple models and sensitizes cancer cells to treatment with other targeted agents. Administration of TP-0903 either as a single agent or in combination with BTK inhibitors may be effective in treating patients with CLL.
| Target | Value |
|
Axl
(Cell-free assay) | 27 nM |
在胰腺癌细胞(PSN-1)中，TP-0903表现出强烈的抗增殖活性，IC50为6 M。TP-0903通过有效抑制Aurora A和B，诱导强烈的G2/M阻滞。在来自CLL患者的CLL B细胞中，TP-0903通过靶向作用于磷酸化Axl，剂量依赖性诱导大量细胞凋亡，并且克服了CLL BMSC-介导的对CLL B细胞凋亡的保护作用。
在成年大鼠海马体中，SAG (2.5 nM)的脑室内给药显著增加新生细胞的数量，并延长海马细胞的生存。在小鼠中，SAG (20 μg/g, i.p.)有效防止GC-诱导的新生儿小脑发育异常。用途
一种高效性的、选择性的Axl受体酪氨酸激酶抑制剂，IC50：27nM。Dubermatinib is a potent and selective AXL inhibitor. TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges. Combination of TP-0903 with BTK inhibitors augments CLL B-cell apoptosis AXL overexpression is a reoccurring theme observed in multiple tumor types that have acquired resistance to various agents. Treatment of cancer cells with TP-0903 reverses the mesenchymal phenotype in multiple models and sensitizes cancer cells to treatment with other targeted agents. Administration of TP-0903 either as a single agent or in combination with BTK inhibitors may be effective in treating patients with CLL.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12963 | Dubermatinib | 1 mg | 293元 | |
| 2024/04/30 | HY-12963 | TP-0903 Dubermatinib | 1341200-45-0 | 2mg | 550元 |