Masitinib
作者：齊岳
發布時間：2023-08-25
09:06:55
點擊數：
產品名稱：Masitinib
產品描述：
| 產品描述 | Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011. |
| 靶點活性 | PDGFRβ:800 nM, PDGFRα:540 nM, Kit:200 nM, Abl1:1.20 μM, Lyn B:510 nM |
| 體外活性 | 與安慰劑相比,Masitinib（12.5 mg/kg/d PO）可增加狗的總體TTP（進展時間）.在表達Δ27的Ba/F3 移植瘤模型中,30 mg/kg Masitinib抑制生長和提高平均存活時間,沒有心臟毒性或遺傳毒性.Masitinib和吉西他濱聯用表現出對抗吉西他濱的細胞系Mia Paca2和Panc1增殖的協同抑制作用. |
| 體內活性 | Masitinib抑制表達人類野生型KIT的Ba/F3的細胞中干細胞因子誘導的細胞增殖,IC50為150 nM,而抑制IL-3刺激的增殖時,IC50值約>10 μM。Masitinib在表達PDGFR-α的Ba/F3細胞中,抑制PDGF-BB刺激的增殖和 PDGFR-α 酪氨酸磷酸化作用,IC50為300 nM。Masitinib濃度≤500 nM時為ATP競爭性抑制劑。Masitinib也有效抑制重組PDGFR和胞內激酶Lyn及FGFR 3。 然而,Masitinib對ABL和c-Fms抑制效果很弱。在哺乳動物細胞系和BMMC中,馬西替尼還能抑制SCF刺激的人Kit酪氨酸磷酸化。Masitinib抑制Ba/F3細胞中KIT獲得的功能突變,包括V559D突變和Δ27鼠突變,IC50分別為3和5 nM。在兩種新型ISS細胞系中,Masitinib抑制細胞生長和PDGFR磷酸化,這表明Masitinib顯示針對原發性和轉移性ISS細胞系的活性,并可能有助于ISS的臨床管理。Masitinib對脫顆粒,細胞因子產生和骨髓肥大細胞遷移的抑制效果比imatinib強很多。Masitinib抑制肥大細胞瘤細胞系包括 HMC-1α155和FMA3的細胞增殖,IC50分別為10和30 nM。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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. (Only for Reference) |
| 別名 | AB1010, 馬賽替尼 |
| 分子量 | 498.65 |
| 分子式 | C28H30N6OS |
| CAS No. | 790299-79-5 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 93 mg/mL (186.5 mM)
H2O: <1 mg/mL
Ethanol: 4 mg/mL (8.02 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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