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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 兔 豚鼠 仓鼠 狗
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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