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Masitinib 马赛替尼

目录号 M1838 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 2/3。

Masitinib结构式

别名:AB1010

包装 价格 库存状态
Free Sample (0.5-1 mg)  原价 ¥ 0
促销价 ¥ 0
中国库存现货
5mg 原价 ¥ 300
促销价 ¥ 285
中国库存现货
10mg 原价 ¥ 400
促销价 ¥ 380
中国库存现货
25mg 原价 ¥ 800
促销价 ¥ 760
中国库存现货
50mg 原价 ¥ 1150
促销价 ¥ 1092.5
中国库存现货
100mg 原价 ¥ 1750
促销价 ¥ 1662.5
中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 2/3。Masitinib浓度≤500 nM时为ATP竞争性抑制剂。Masitinib也有效抑制重组PDGFR和胞内激酶Lyn, 及FGFR 3。 然而, Masitinib 对ABL和c-Fms抑制效果很弱。

使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Blood (2018). Figure 5. Masitinib (Abmole Bioscience)
方法 BCR signaling repre
细胞系/动物模型 923 cells lines
浓度 2.5 μM, 5 μM or 10 μM
处理时间 72 h
实验结果 We observed a consistent reduction of the tumor mass in animals treated with masitinib
数据来源 Res Vet Sci (2014). Figure 2. Masitinib
方法 Clonogenic assays
细胞系/动物模型 JB, KH and Hamilton ISS cells
浓度 6 μM
处理时间 24 h
实验结果 There were no differences in radiosensitivity between control cells (0 lM masitinib) and those treated with 1 μM masitinib regardless of radiation dose (JB p = 0.56; KH p = 0.7; Hamilton p = 0.11); due to these comparable findings, the assay was performed only once
数据来源 Res Vet Sci (2014). Figure 1. Masitinib
方法 Clonogenic assays
细胞系/动物模型 JB, KH and Hamilton ISS cells
浓度 6 μM
处理时间 24 h
实验结果 For each cell line, there were no significant differences in ISS radiosensitivity between control cells (0 μM masitinib) and those treated with 6 μM masitinib at any radiation dose (JB p = 0.11; KH p = 0.07; Hamilton p = 0.8)
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 Ba/F3 cell
方法 For the assay of Ba/F3 cell proliferation, microtitre plates were seeded with a total of 104 cells/well in 100 µl of RPMI 1640 medium with 10% foetal bovine serum at 37°C. These were supplemented, or not, with either 0.1% conditioned medium from X63-IL-3 cells or 250 ng/ml murine SCF. The murine SCF, which activates KIT, was purified from the conditioned medium of SCF-producing CHO cells (gift of S. Lyman, Immunex). Cells were grown for 48 hours at 37°C and then incubated with 10 µl/well of WST-1 reagent (Roche Applied Science, France) for 3 hours at 37°C. The amount of formazan dye formed was quantified by its absorbance at 450 nm using a scanning multiwell spectrophotometer (MultiSkan MS, Thermo-LabSystems, France). A blank well without cells was used as a background control for the spectrophotometer and all assays were performed in triplicate.
浓度 0~10 μM
处理时间 48 h
动物实验
动物模型 Ba/F3 Δ27 tumour model in Female MBRI Nu/Nu mice
配制 placebo
剂量 10, 30, or 45 mg/kg twice daily for 10 days
给药处理 orally
化学数据
分子量 498.64
分子式 C28H30N6OS
CAS号 790299-79-5
溶解性(25°C) DMSO ≥100 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

以下数据基于产品分子量,对于具体产品,请根据在不同溶剂中的溶解度和COA中的说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.0055 mL 10.0273 mL 20.0545 mL
5 mM 0.4011 mL 2.0055 mL 4.0109 mL
10 mM 0.2005 mL 1.0027 mL 2.0055 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
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,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Klopfleisch et al. BMC Vet Res. Transcriptome and proteome analysis of tyrosine Kinase inhibitor treated canine mast cell tumour cells identifies potentially kit signaling-dependent genes.

[2] Lyles et al. Vet Comp Oncol. In vitro effects of the tyrosine kinase inhibitor, masitinib mesylate, on canine hemangiosarcoma cell lines.

[3] Lee-Fowler et al. Int Arch Allergy Immunol. The tyrosine kinase inhibitor masitinib blunts airway inflammation and improves associated lung mechanics in a feline model of chronic allergic asthma.

[4] Georgin-Lavialle et al. Eur J Haematol. Mast cell leukemia: identification of a new c-Kit mutation, dup(501-502), and response to masitinib, a c-Kit tyrosine kinase inhibitor.

[5] Lawrence et al. Vet Comp Oncol. Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells.

[6] Dubreuil P, et al. PLoS One. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.

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关键词:Masitinib, AB1010, Masitinib供应商, VEGFR/PDGFR抑制剂, 购买Masitinib, Masitinib溶解度, Masitinib结构式








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