Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pexidartinib (PLX-3397) 是具有口服活性的选择性ATP-竞争性的集落刺激因子 1 和c-Kit 抑制剂,IC50值分别为 20 和 10 nM。它可诱导细胞凋亡,具有抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 217 | 现货 | ||
5 mg | ¥ 493 | 现货 | ||
10 mg | ¥ 671 | 现货 | ||
25 mg | ¥ 1,190 | 现货 | ||
50 mg | ¥ 1,970 | 现货 | ||
100 mg | ¥ 3,330 | 现货 | ||
200 mg | ¥ 4,150 | 现货 | ||
500 mg | ¥ 6,620 | 现货 | ||
1 g | ¥ 8,660 | 现货 | ||
2 g | ¥ 11,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 540 | 现货 |
产品描述 | Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity. |
靶点活性 | FLT3:160 nM, Kit:10 nM, CSF-1R:20 nM |
体外活性 | In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. [1] |
体内活性 | In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C?Ly6 g?F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. [1] In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. [2] In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. [3] In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. [4] |
激酶实验 | Competitive binding fluorescent polarization assay: Recombinant Hsp90β, TAMRA-radicicol, or various concentrations of NVP-BEP800 is added in assay buffer (50 mM TRIS pH 7.4, 5 mM MgCl2, 150 mM KCl, and 0.1% CHAPS), mixed, and incubated at room temperature for 30 to 45 minutes prior to reading. The 2D-FIDA-based HTS assay based on confocal technologies monitors the decreased fluorescence polarization on displacement of the high affinity ligand TAMRA-radicicol from Hsp90β by NVP-BEP800. The concentration of NVP-BEP800 which inhibits Hsp90β by 50% is determined from the competition curve. |
别名 | PLX-3397 |
分子量 | 417.81 |
分子式 | C20H15ClF3N5 |
CAS No. | 1029044-16-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 77 mg/mL (184.3 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3934 mL | 11.9672 mL | 23.9343 mL | 59.8358 mL |
5 mM | 0.4787 mL | 2.3934 mL | 4.7869 mL | 11.9672 mL | |
10 mM | 0.2393 mL | 1.1967 mL | 2.3934 mL | 5.9836 mL | |
20 mM | 0.1197 mL | 0.5984 mL | 1.1967 mL | 2.9918 mL | |
50 mM | 0.0479 mL | 0.2393 mL | 0.4787 mL | 1.1967 mL | |
100 mM | 0.0239 mL | 0.1197 mL | 0.2393 mL | 0.5984 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pexidartinib 1029044-16-3 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors c-Fms FLT CSF-1R c-Kit inhibit CSF-1 receptor SCFR Inhibitor PLX 3397 PLX3397 colony stimulating factor 1 receptor CSF1R CD117 PLX-3397 inhibitor