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TP-0903是一种有效的选择性的AXL受体酪氨酸激酶抑制剂，IC50 为 27 nM。
TP-0903是一种有效的选择性的AXL受体酪氨酸激酶抑制剂，IC50 为 27 nM。
体外研究表明，TP-0903在胰腺癌细胞(PSN-1)中，表现出强烈的抗增殖活性，IC50值为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。
| 细胞实验 | |
|---|---|
| 细胞系 | PSN-1 cells |
| 方法 | For cell proliferation assays, 45 µL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate cell growth media containing 10% FBS and incubated overnight at 37 °C and 5% CO2. The following day, test compounds are diluted in serum free growth media to 10x desired concentrations and 5 µL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 µL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an EnVision microplate reader. Percent cell viability for test compounds is calculated by comparing treated wells to appropriate controls (e.g. vehicle treated) included on each plate. |
| 浓度 | |
| 处理时间 | 96 hours |
| 动物实验 | |
|---|---|
| 动物模型 | Female nude mice (6 weeks old) carrying GBM cells |
| 配制 | - |
| 剂量 | 20 mg/kg/d |
| 给药处理 | tail vein injection |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
| 分子量 | 516.06 |
| 分子式 | C24H30ClN7O2S |
| CAS号 | 1341200-45-0 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 3 mg/mL warmed |
| 储存和运输条件 |
固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.9378 mL | 9.6888 mL | 19.3776 mL |
| 5 mM | 0.3876 mL | 1.9378 mL | 3.8755 mL |
| 10 mM | 0.1938 mL | 0.9689 mL | 1.9378 mL |
CNS Neurosci Ther. 2020 Jul;26(7):777.
Retraction: Receptor tyrosine kinase AXL is correlated with poor prognosis and induces temozolomide resistance in glioblastoma
TP-0903购买自AbMole
CNS Neurosci Ther. 2019 Oct 2.
Receptor tyrosine kinase AXL is correlated with poor prognosis and induces temozolomide resistance in glioblastoma.
TP-0903购买自AbMole
 |
数据来源 | CNS Neurosci Ther (2020 Jul). Figure 5.TP-0903 (Abmole Bioscience, TX, USA) |
| 方法 | In vitro cell viability assay | |
| 细胞系 | GBM cells | |
| 浓度 | different concentrations | |
| 处理时间 | 3 days | |
| 实验结果 | Moreover, an in vitro proliferation assay indicated that TP-0903 attenuated the growth of TMZ-resistant U87 cells, and more importantly, the gained TMZ resistance was significantly reversed by TP-0903. |
Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors.
Sinha S, et al. Clin Cancer Res. 2015 May 1;21(9):2115-26. PMID: 25673699.
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