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CAS No.: 1037624-75-1

Bemcentinib/贝森替尼 Catalog No. CSN17144

Synonyms: R428;BGB324

R428 is a potent and selective small-molecule inhibitor (IC50=14 nM), and blocks the activities of Axl.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Axl

IC50:14nM
描述Axl is a member of the TAM (Tyro3, Axl, Mer) receptor tyrosine kinase (RTK) family and Axl signaling stimulates cellular responses and results in invasion, migration, survival signaling, angiogenesis, cell transformation, and proliferation associated with cancer. R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM by blocking the catalytic and procancerous activities with low nanomolar activity. R428-treated tumors reduce expression of the cytokine granulocyte macrophage colony-stimulating factor and angiogenesis in corneal micropocket and tumor model as well as metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopicmouse models of breast cancer. The mean IC50 for the primary CLL B cells is of ~2.0 μM of R428 treatment and no significant amount of cell death of normal B-, T-, natural killer (NK) cells were observed at this dose of 2.5 μM. R428 inhibited Axl phosphorylation by 50%-60% in CLL B cells at a dose of 1.0 μM for overnight suggesting R428 can target Axl phosphorylation and are responsible for apoptosis induction in CLL B cells. Furthermore, a substantial level of reduction in Mcl-1 in all the 3 CLL B-cell lysates (P5-P7) treated with R428 in both a dose- and time dependent manner. Besides, R428 inhibited growth of H1299 with an IC50 of approximately 4 μM while LDC1267 had no effects on the cell growth even at 20 μM. R428 induced a series of apoptotic events, including caspase-8/9 activation, PARP cleavage, and upregulation of anti-apoptotic proteins Bcl-xl and Bcl-2 in the Hela cells. R428 treatment also increased the autophagy level of LC3-II, indicating the induction of autophagy initiation, but did not decrease the level of p62, suggesting a blockage of autophagic degradation. Further analyses revealed that R428 blocked lysosomal acidification and recycling, accumulated autophagosomes and lysosomes, and induced cell apoptosis.

动物研究

剂量

Nude Mice: 7 mg/kg - 125 mg/kg^[3] (p.o.) BALB/c Mice: 7 mg/kg - 75 mg/kg^[3] (p.o.) C57BL/6 Mice: 50 mg/kg, 100 mg/kg^[4] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Mice^[3]
Dose	75 mg/kg
Administration	p.o.
C_max	6.8 µmol/l
T_1/2	13 h

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9738 mL
- 9.8689 mL
- 19.7377 mL
- 5 mM
- 0.3948 mL
- 1.9738 mL
- 3.9475 mL
- 10 mM
- 0.1974 mL
- 0.9869 mL
- 1.9738 mL

技术信息

CAS号

1037624-75-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H34N8

运输

蓝冰

分子量

506.64

别名

R428;BGB324

溶解度

DMSO	6.0 mg/mL (11.8 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+corn oil

1 mg/mL

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