製品番号: HY-10209A

Masitinib mesylate

(別名: AB-1010 mesylate)

6 Cited Publications

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

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.

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純度: 99.98%
CAS 番号: 1048007-93-7
分子式: C₂₉H₃₄N₆O₄S₂
分子量:594.75

保管条件:

4°C, sealed storage, away from moisture

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

Masitinib mesylate 構造式

CAS 番号: 1048007-93-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (6)
溶剤 & 溶解度
- 体外
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
Bioz

生物活性

製品説明

IC₅₀ & Target

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

PDGFR アイソフォーム固有の製品をすべて表示 :

Src アイソフォーム固有の製品をすべて表示 :

体外実験

Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. Masitinib demonstrates weak inhibition of Abl and c-Fms. Masitinib more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration than imatinib. In Ba/F3 cells expressing human wild-type Kit, masitinib inhibits SCF (stem cell factor)-induced cell proliferation with an IC₅₀ of 150 nM, while the IC₅₀ for inhibition of IL-3-stimulated proliferation is at approximately >10 μM. In Ba/F3 cells expressing PDGFRα, masitinib inhibits PDGF-BB-stimulated proliferation and PDGFRα tyrosine phosphorylation with IC₅₀ of 300 nM. Masitinib also causes inhibition of SCF-stimulated tyrosine phosphorylation of human Kit in mastocytoma cell-lines and BMMC. Masitinib inhibits Kit gain-of-function mutants, including V559D mutant and Δ27 mouse mutant with IC₅₀ of 3 and 5 nM in Ba/F3 cells. Masitinib inhibits the cell proliferation of mastocytoma cell lines including HMC-1α155 and FMA3 with IC₅₀ of 10 and 30 nM, respectively^[1].
Masitinib inhibits cell growth and PDGFR phosphorylation in two novel ISS cell lines, which suggest that Masitinib displays activity against both primary and metastatic ISS cell line and may aid in the clinical management of ISS^[2].

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

体内実験

Masitinib inhibits tumour growth and increases the median survival time in Δ27-expressing Ba/F3 tumor models at 30 mg/kg, without cardiotoxicity or genotoxicity^[1].
Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs^[3].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1048007-93-7
性状 Solid
分子量 594.75
分子式 C₂₉H₃₄N₆O₄S₂
Color White to yellow
SMILES

O=C(NC1=CC=C(C(NC2=NC(C3=CC=CN=C3)=CS2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4.CS(=O)(O)=O
別名

AB-1010 mesylate
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

Publications (6)

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Journal Impact Factor

Science

Replication and single-cycle delivery of SARS-CoV-2 replicons. [Abstract]

2021 Nov 26;374(6571):1099-1106. PMID: 34648371
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Ecotoxicol Environ Saf

Dibutyl phthalate promotes central precocious puberty through primordial follicle activation by downregulating BMP15. [Abstract]

2025 Jun 4:300:118460. PMID: 40472697
Eur J Pharmacol

Therapeutic effects of masitinib on abnormal mechanoreception in a mouse model of tourniquet-induced extremity ischemia-reperfusion. [Abstract]

2021 Nov 15:911:174549. PMID: 34619116
BMC Vet Res

The secondary KIT mutation p.Ala510Val in a cutaneous mast cell tumour carrying the activating mutation p.Asn508Ile confers resistance to masitinib in dogs. [Abstract]

2020 Feb 19;16(1):64. PMID: 32075643
University of Heidelberg

2025.

溶剤 & 溶解度

体外:

1M HCl : 100 mg/mL (168.14 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : ≥ 30 mg/mL (50.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6814 mL

8.4069 mL

16.8138 mL

5 mM

0.3363 mL

1.6814 mL

3.3628 mL

10 mM

0.1681 mL

0.8407 mL

1.6814 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass

濃度

体積

分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始)

体積 _(開始)

濃度 _(終了)

体積 _(終了)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

プロトコル

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 K_m 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.

MedChemExpress (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.

MedChemExpress (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).

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (280 KB)
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- Deutsch - DE (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Dubreuil P, et al. Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT. PLoS One, 2009, 4(9), e7258.

[2]. Lawrence J, et al. Masitinib demonstrates anti-proliferative and pro-apoptotic activity in primary and metastatic feline injection-site sarcoma cells. Vet Comp Oncol, 2011, doi: 10.1111/j.1476-5829.2011.00291.x. [Content Brief]

[3]. Hahn KA, et al. Masitinib is safe and effective for the treatment of canine mast cell tumors. J Vet Intern Med, 2008, 22(6), 1301-1309. [Content Brief]

[4]. Marech I, et al. Masitinib (AB1010), from canine tumor model to human clinical development: where we are? Crit Rev Oncol Hematol. 2014 Jul;91(1):98-111. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Keywords

Masitinib mesylate

6 Cited Publications

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Masitinib mesylate

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MedChemExpress（MCE）の使用を引用している文献 Masitinib mesylate

PDGFR アイソフォーム固有の製品をすべて表示

Src アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (6)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Masitinib mesylate 関連分類

製品番号: HY-10209A