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Masitinib mesylate

(Synonyms: 甲磺酸马赛替尼; AB-1010 mesylate)

目录号: PL01346 纯度: ≥99%

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-Kit，IC50 =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 FGFR3 和 FAK。Masitinib mesylate (AB-1010 mesylate) 有抗增殖，促凋亡活性，且毒性低。

CAS No. :1048007-93-7

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中文名称	Masitinib mesylate
中文别名	4-[(4-甲基-1-哌嗪基)甲基]-N-[4-甲基-3-[[4-(3-吡啶基)-2-噻唑基]氨基]苯基]-甲基磺酰基苯胺;马赛替尼;马赛替尼甲磺酸盐;甲磺酸马赛替尼
英文名称	Masitinib mesylate
英文别名	4-(4-Methylpiperazin-1-ylmethyl)benzoic Acid;4-((4-METHYLPIPERAZIN-1-YL)METHYL)BENZOIC ACID;SBB063308;4-(4-carboxybenzyl)-1-methylpiperazine;ACMC-1BSQT;4-(4-methylpiperazinomethyl)benzoic acid;4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-phenyl]-benzamide methanesulfonate;SureCN65179;4-(4-methyl-piperazin-1-ylmethyl)benzoic acid;Masitinib mesylate;4-(4-methyl-piperazine-1-ylmethyl)-benzoic acid;AG-D-20558;Benzoic acid,4-[(4-methyl-1-piperazinyl)methyl]-;4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)-1,3-thiazol-2-yl]amino}phenyl)benzamide mesylate;Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]-, methanesulfonate;Masitinib (mesylate);methanesulfonic acid,4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide;4-(4-methylpiperazin-1-ylmethyl);4-[(4-methylpiperazin-1-yl)methyl]-n-[4-methyl-3-[(4-pyridin-3-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide;AB1010 mesylate;AB-1010 mesylate;Methanesulfonic Acid;4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide methanesulfonate (1:1);Masivet Mesylate;ZK89EG3A18;Kinavet;Masitinib mesilate;Masitinibmesylate;AB 1010 mesylate;C28H30N6OS.CH4O3S;TXCWBWKVIZGWEQ-UHFFFAOYSA-N;3415AH;SB14845;Benzamide, 4-((4-methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-thiazolyl)amino)phenyl)-, m
Cas No.	1048007-93-7
分子式	C₂₉H₃₄N₆O₄S₂
分子量	594.75
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	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-Kit，IC50 =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 FGFR3 和 FAK。Masitinib mesylate (AB-1010 mesylate) 有抗增殖，促凋亡活性，且毒性低。

产品详情

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-Kit，IC₅₀=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 FGFR3 和 FAK。Masitinib mesylate (AB-1010 mesylate) 有抗增殖，促凋亡活性，且毒性低。

生物活性

Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC 50 =200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC 50 s=540/800 nM), Lyn (IC 50 = 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.

性状

Solid

IC50 & Target[1][2]

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

体外研究(In Vitro)

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 phospho

体内研究(In Vivo)

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.
Masitinib (12.5 mg/kg/d, p.o.) increases overall TTP (time-to-tumor progression) compared with placebo in dogs. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: 1M HCl : 100 mg/mL (168.14 mM; ultrasonic and adjust pH to 1 with HCl)DMSO : ≥ 30 mg/mL (50.44 mM)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Masitinib mesylate

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