Masitinib (AB1010)


Masitinib (AB1010)化学構造


Masitinib (AB1010)は一種の新たなKitとPDGFRα/β阻害剤で、IC50値が200 nMと540 nM/800 nMに分かれることです。Masitinib (AB1010)はABLとc-Fmsを抑制する効果が少し弱いです。臨床3期。

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  • H&E stained histology slides of A), C), and E) control implants and B), D), and F) drug-loaded implants for 14, 21 and 28 day time points respectively. Location of the implants is denoted by the asterisk ‘*’. Scale bar: 200 μm.

    Biomaterials 2013 34, 9737-46. Masitinib (AB1010) purchased from Selleck.




製品説明 Masitinib (AB1010)は一種の新たなKitとPDGFRα/β阻害剤で、IC50値が200 nMと540 nM/800 nMに分かれることです。Masitinib (AB1010)はABLとc-Fmsを抑制する効果が少し弱いです。臨床3期。
特性 Potential low side-effect profile.
Kit [1] Lyn B [1] PDGFRα [1] PDGFRβ [1] Abl1 [1]
200 nM 510 nM 540 nM 800 nM 1.20 μM
In vitro試験

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. In contrast, 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]

In vivo試験 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 PO) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. [3] The combination of masitinib/gemcitabine shows synergy in vitro on proliferation of gemcitabine-refractory cell lines Mia Paca2 and Panc1, and to a lesser extent on Mia Paca-2 pancreatic tumours in Nog璖CID mice. [4]


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In vitro enzyme-linked immunoassay with recombinant protein kinases:

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 5 M urea 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.
細胞アッセイ: [1]
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  • 細胞株: Ba/F3 cells expressing wild-type or mutant human Kit, HMC1, HMC-1α155
  • 濃度: 0.1 nM - 10 μM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
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  • 動物モデル: Ba/F3 Δ27 tumour model in female MBRI Nu/Nu mice
  • 製剤: DMSO
  • 投薬量: 30 mg/kg (intraperitoneal) or 10, 30, or 45 mg/kg (orally).
  • 投与方法: Intraperitoneal or orally administered.

溶解度 (25°C)

体外 DMSO 100 mg/mL (200.54 mM)
Ethanol 4 mg/mL (8.02 mM)
Water <1 mg/mL
体内 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 30mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 498.64


CAS No. 790299-79-5
in solvent
別名 N/A





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02490488 Active, not recruiting Ovarian Cancer AB Science April 2014 Phase 2
NCT02605044 Recruiting 2nd Line Metastatic Colorectal Cancer AB Science January 2014 Phase 3
NCT02009423 Unknown status Gastro-Intestinal Stromal Tumour AB Science January 2014 Phase 3
NCT02588677 Active, not recruiting Amyotrophic Lateral Sclerosis (ALS) AB Science April 2013 Phase 2|Phase 3
NCT01694277 Unknown status Gastrointestinal Stromal Tumors AB Science April 2012 Phase 3
NCT01433497 Unknown status Multiple Sclerosis, Secondary Progressive|Multiple Sclerosis, Primary Progressive|Multiple Sclerosis, Relapse Free AB Science August 2011 Phase 2|Phase 3



Handling Instructions


  • * 必須


c-Kit Inhibitors with Unique Features


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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID