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Bemcentinib

Bemcentinib

产品编号 T6269   CAS 1037624-75-1
别名: R428, BGB324

Bemcentinib (R428) 是具有选择性的、高效的 Axl 抑制剂,其 IC50=14 nM。

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Bemcentinib Chemical Structure
Bemcentinib, CAS 1037624-75-1
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
产品目录号及名称: Bemcentinib (T6269)
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选择批次  
纯度: 99.8%
纯度: 99.73%
纯度: 98.71%
纯度: 98%
纯度: 97.03%
纯度: 97%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

T6269_2

Crystal structure of JAK2 JH2 in complex with Bemcentinib

分子量 506.64
分子式 C30H34N8
CAS No. 1037624-75-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 10 mg/mL(19.7 mM)

溶液配制表

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

计算器

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稀释计算器
配液计算器
分子量计算器
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参考文献

1. Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54. 2. Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice. J Pharmacol Exp Ther. 2011 May;337(2):457-64. 3. Ghosh AK, et al. The novel receptor tyrosine kinase Axl is constitutively active in B-cell chronic lymphocytic leukemia and acts as a docking site of nonreceptor kinases: implications for therapy. Blood. 2011 Feb 10;117(6):1928-37.

文献引用

1. Huang M, Liu M, Huang D, et al. Tumor perivascular cell-derived extracellular vesicles promote angiogenesis via the Gas6/Axl pathway. Cancer Letters. 2021 2. Yuan Y, Guo Y, Guo Z W, et al.Marsdenia tenacissima extract induces endoplasmic reticulum stress-associated immunogenic cell death in non-small cell lung cancer cells through targeting AXL.Journal of Ethnopharmacology.2023: 116620.
Tepotinib UNC2025 2HCl (1429881-91-3(free base)) Gilteritinib hemifumarate AXL-IN-13 AXL-IN-14 UNC569 2-(Chloromethyl)-4-(4-nitrophenyl)thiazole R916562

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 酪氨酸激酶分子库 抗癌临床化合物库 高选择性抑制剂库 抗癌药物库 药物功能重定位化合物库 临床期小分子药物库 人代谢物化合物库 表型筛选靶点鉴定库 抗癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
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技术支持

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。

Keywords

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

 

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