Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bemcentinib (R428) 是具有选择性的、高效的 Axl 抑制剂,其 IC50=14 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 415 | 现货 | ||
2 mg | ¥ 623 | 现货 | ||
5 mg | ¥ 1,150 | 现货 | ||
10 mg | ¥ 1,950 | 现货 | ||
25 mg | ¥ 2,990 | 现货 | ||
50 mg | ¥ 3,912 | 现货 | ||
100 mg | ¥ 5,920 | 现货 | ||
200 mg | ¥ 8,190 | 现货 | ||
500 mg | ¥ 12,100 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,150 | 现货 |
产品描述 | Bemcentinib (R428) is a selective inhibitor of Axl (IC50: 14 nM) and has been investigated for the treatment of NSCLC. |
靶点活性 | Axl:14 nM (cell free) |
体外活性 | Bemcentinib (R428) activity was limited to the tyrosine kinase subfamily. Of the 133 kinases, Axl was most potently inhibited by R428. With the exception of Tie-2, Ftl-1, Flt-3, Ret, and Abl, kinase inhibition by R428 was at least 10 times lower than observed for Axl. R428 dose-dependently suppressed invasion of both human MDA-MB-231 and murine 4T1 breast cancer cell lines [1]. Addition of R428 (50 nM-1 μM) resulted in a dose-dependent inhibition of differentiation of 3T3-F442A preadipocytes into mature adipocytes. Oil Red O staining ranged between 84 and 35% of that of DMSO control at R428 concentrations between 50 nM and 1 μM. Inhibition of Axl signaling by R428 in differentiating preadipocytes was confirmed by the Axl cell-based assay, yielding lower values (A450) for phospho-Akt activity upon treatment with 1 μM R428 compared with medium control or DMSO control [2]. The Axl inhibitor R428 showed a mean IC50 dose of ~ 2.0μM for the primary CLL B cells after 24 hours of treatment and normal B-, T- and natural killer (NK) cells showed no significant amount of cell death at this dose of R428 (2.5μM) under similar experimental conditions [3]. |
体内活性 | R428 treatment reduced lung metastasis. R428 (7 mg/kg twice daily) significantly suppressed both total metastatic burden and the number of larger metastases. R428 suppressed both tumor angiogenesis and vascular endothelial growth factor (VEGF)–induced corneal neovascularization in vivo [1]. At day 35, the last day of HFD feeding, the body weight in both groups treated with R428 (75 mg/kg/day or 25 mg/kg twice daily, p.o.) was significantly lower than in the corresponding vehicle-treated groups. Compared with the start of the experiment, body weights at the end were significantly increased in both vehicle-treated groups, but not in R428-treated groups [2]. |
激酶实验 | A five-point R428 dose titration was performed in radiometric in vitro kinase assays on 133 kinases at the Km(ATP) for each kinase. Axl, Mer, and Tyro3 assays were also performed using a fluorescence polarization protocol. HER2 activity was determined by Z'-LYTE assay [1]. |
细胞实验 | MDA-MB-231 or 4T1 cells (1 × 10^5) were allowed to migrate through Matrigel toward 20% FCS in an 8-μm pore 24-well Transwell plate at 37°C for 16 to 24 h. Noninvaded cells and Matrigel were removed by swabbing. Invaded cells were fixed in 4% formaldehyde, stained with 1% crystal violet, and quantified as for Axl cell-based assay. Cells were preincubated with R428 for 3 h. R428 was added to both upper and lower Transwell chambers [1]. |
动物实验 | Female BALB/c mice were inoculated in the mammary fat pad with 0.5 × 10^6 4T1 cells. Forty-eight hours after inoculation, mice were randomized into treatment groups (n = 10). Oral dosing with R428 (7–75 mg/kg twice daily) or vehicle continued until days 19 to 21. Cisplatin (1.2 or 4 mg/kg) was administered i.v. once weekly. Body weight and tumor size were measured thrice per week. Lungs were exposed postmortem. Total number and size of surface lung macrometastases were measured (small, <2 mm; medium, ≥2 mm and <3 mm; large, ≥3 mm). Half of each primary tumor was snap frozen in liquid nitrogen. The other half, and the livers were fixed in paraformaldehyde/lysine/periodate solution, paraffin embedded and sectioned (5 μm thick). Two H&E-stained liver sections per animal were examined microscopically for micrometastases in three view fields. Synergism was determined using Clark's synergy calculation [1]. |
别名 | R428, BGB324 |
化合物与蛋白结合的复合物 |
Crystal structure of JAK2 JH2 in complex with Bemcentinib |
分子量 | 506.64 |
分子式 | C30H34N8 |
CAS No. | 1037624-75-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 10 mg/mL(19.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9738 mL | 9.8689 mL | 19.7379 mL | 49.3447 mL |
5 mM | 0.3948 mL | 1.9738 mL | 3.9476 mL | 9.8689 mL | |
10 mM | 0.1974 mL | 0.9869 mL | 1.9738 mL | 4.9345 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。
Bemcentinib 1037624-75-1 Tyrosine Kinase/Adaptors TAM Receptor R428 Tyro3 Mer Inhibitor BGB324 BGB 324 R 428 BGB-324 Axl inhibit R-428 inhibitor