1. Protein Tyrosine Kinase/RTK Apoptosis
  2. c-Kit PDGFR Src FGFR Apoptosis
  3. Masitinib mesylate

Masitinib mesylate  (Synonyms: 甲磺酸马赛替尼; AB-1010 mesylate)

目录号: HY-10209A 纯度: 99.83%
COA 产品使用指南

Masitinib mesylate (AB-1010 mesylate) 是一种有效的,生物口服可利用的,且选择性的 c-Kit 抑制剂 (对于人重组 c-KitIC50 =200 nM),它还抑制 PDGFRα/β (IC50s=540/800 nM),Lyn (对 LynB 的 IC50=510 nM),Lck,较小程度上抑制 FGFR3FAK。Masitinib mesylate (AB-1010 mesylate) 有抗增殖,促凋亡活性,且毒性低。

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Masitinib mesylate Chemical Structure

Masitinib mesylate Chemical Structure

CAS No. : 1048007-93-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥440
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5 mg ¥250
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10 mg ¥400
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50 mg ¥1200
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100 mg ¥1850
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200 mg ¥2850
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500 mg   询价  
1 g   询价  

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Other Forms of Masitinib mesylate:

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity[1][2][4].

IC50 & Target

IC50: 200 nM (Kit), 540 nM (PDGFRα), 800 nM (PDGFRβ), 510 nM (LynB)[1]

体外研究
(In Vitro)

Masitinib 在浓度≤500 nM 时,是一种针对 ATP 的竞争性抑制剂。Masitinib 还有效抑制重组 PDGFR 和细胞内激酶 Lyn,并在较小程度上抑制成纤维细胞生长因子受体 3。相比之下,Masitinib 表现出对 Abl 和 c-Fms 的弱抑制。与伊马替尼相比,Masitinib 更强烈地抑制脱颗粒、细胞因子产生和骨髓肥大细胞迁移。在表达人野生型 Kit 的 Ba/F3 细胞中,Masitinib 抑制 SCF (干细胞因子) 诱导的细胞增殖,IC50 为 150 nM,而 IC50抑制 IL-3 刺激的增殖的浓度约为 >10 μM。在表达 PDGFRα 的 Ba/F3 细胞中,Masitinib 抑制 PDGF-BB 刺激的增殖和 PDGFRα 酪氨酸磷酸化,IC50 为 300 nM。Masitinib 还抑制肥大细胞瘤细胞系和 BMMC 中 SCF 刺激的人 Kit 酪氨酸磷酸化。Masitinib 抑制 Kit 功能获得突变体,包括 V559D 突变体和 Δ27 小鼠突变体,在 Ba/F3 细胞中的 IC50 分别为 3 和 5 nM。Masitinib 抑制包括 HMC-1α155 和 FMA3 在内的肥大细胞瘤细胞系的细胞增殖,IC50 分别为 10 和 30 nM[1]
两种新型 ISS 细胞系的生长和 PDGFR 磷酸化,这表明 Masitinib 显示出针对原代和转移性 ISS 细胞系的活性,可能有助于 ISS 的临床管理[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Masitinib mesylate (30 mg/kg) 抑制肿瘤生长并增加表达 Δ27 的 Ba/F3 肿瘤模型的中位生存时间,而无心脏毒性或遗传毒性[1]
Masitinib mesylate (12.5 mg/kg/d,po) 与安慰剂相比,肿瘤进展时间增加[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

594.75

Formula

C29H34N6O4S2

CAS 号
性状

固体

颜色

White to yellow

中文名称

甲磺酸马赛替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

1M HCl 中的溶解度 : 100 mg/mL (168.14 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

DMSO 中的溶解度 : ≥ 30 mg/mL (50.44 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6814 mL 8.4069 mL 16.8138 mL
5 mM 0.3363 mL 1.6814 mL 3.3628 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Kinase Assay
[1]

A 96-well microtitre plateis coated overnight with 0.25 mg/mL poly(Glu,Tyr 4:1), rinsed twice with 250 µL of washing buffer (10 mM phosphate-buffered saline [pH 7.4] and 0.05% Tween 20) and dried for 2 hours at room temperature. Assays are performed at room temperature with a final volume of 50 µL in kinase buffer (10 mM MgCl2, 1 mM MnCl2, 1 mM sodium orthovanadate, 20 mM HEPES, pH 7.8) containing ATP at a concentration of at least twice the Km for each enzyme and an appropriate amount of recombinant enzyme to ensure a linear reaction rate. Reactions are initiated upon introduction of the enzyme and terminated with the addition of one reaction volume (50 μL) of 100 mM EDTA per 5mol/Lurea mix. Plates are washed three times and incubated with 1:30,000 horseradish peroxidase-conjugated anti-phosphotyrosine monoclonal antibody, then washed three times and incubated with tetramethylbenzidine. The final reaction product is quantified by spectrophotometry at 450 nm.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For the assay of Ba/F3 cell proliferation, microtitre plates are seeded with a total of 104 cells/well in 100 μL of RPMI 1640 medium with 10% foetal bovine serum at 37°C. These are 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, is purified from the conditioned medium of SCF-producing CHO cells. Cells are grown for 48 hours at 37°C with masitinib and then incubated with 10 μL/well of WST-1 reagent for 3 hours at 37°C. The amount of formazan dye formed is quantified by its absorbance at 450 nm using a scanning multiwell spectrophotometer. A blank well without cells is used as a background control for the spectrophotometer.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Male Nog-SCID mice (7 weeks old) are under specific pathogen-free conditions at 20±1°C in a 12-hour light/12-hour dark cycle and ad libitum access to food and filtered water. Mia Paca-2 cells are cultured as described above. At day 0 (D0), mice are injected with 107 Mia Paca-2 cells in 200 µL PBS into the right flank. Tumours are allowed to grow for 1.5 to 4 weeks until the desired tumour size is reached (appr 200 mm3). At day 28, animals are allocated into four treatment groups (n=7 to 8 per group), ensuring that each group's mean body weight and tumour volume are well matched. Treatment is then administered for up to 4 weeks, after which time the animals are sacrificed. Treatments consisted of either: a) daily sterile water for the control group, b) an intraperitoneal (i.p.) injection of 50 mg/kg gemcitabine twice a week, c) daily gavage with 100 mg/kg masitinib, or d) combined i.p injection of 50 mg/kg gemcitabine twice a week and daily gavage with 100 mg/kg masitinib. Tumour size is measured with callipers and tumour volume is estimated using the formula: volume=(length×width2)/2. The tumour growth inhibition ratio is calculated as (100)×(median tumour volume of treated group)/(median tumour volume of control group).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / 1M HCl 1 mM 1.6814 mL 8.4069 mL 16.8138 mL 42.0345 mL
5 mM 0.3363 mL 1.6814 mL 3.3628 mL 8.4069 mL
10 mM 0.1681 mL 0.8407 mL 1.6814 mL 4.2034 mL
15 mM 0.1121 mL 0.5605 mL 1.1209 mL 2.8023 mL
20 mM 0.0841 mL 0.4203 mL 0.8407 mL 2.1017 mL
25 mM 0.0673 mL 0.3363 mL 0.6726 mL 1.6814 mL
30 mM 0.0560 mL 0.2802 mL 0.5605 mL 1.4011 mL
40 mM 0.0420 mL 0.2102 mL 0.4203 mL 1.0509 mL
50 mM 0.0336 mL 0.1681 mL 0.3363 mL 0.8407 mL
1M HCl 60 mM 0.0280 mL 0.1401 mL 0.2802 mL 0.7006 mL
80 mM 0.0210 mL 0.1051 mL 0.2102 mL 0.5254 mL
100 mM 0.0168 mL 0.0841 mL 0.1681 mL 0.4203 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Masitinib mesylate
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HY-10209A
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