Imatinib Mesylate (STI571)

• FDA-approved Drug Library
• Bioactive Compound Library
• Anti-cancer Compound Library
• Kinase Inhibitor Library
• Tyrosine Kinase Inhibitor Library
• TGF-beta/Smad Compound Library

• 纯度 = 99.26%

Imatinib Mesylate是一种酪氨酸激酶YZ剂，对v-Abl、c-Kit和PDGFR的IC50值分别为600 nM、100 nM和100 nM。

酪氨酸激酶属于蛋白激酶的子类，在细胞内负责将ATP的磷酸基团转移到蛋白质上。结果表明，酪氨酸激酶在ZL相关疾病中起着关键作用，参与c-Abl、PDGFR或c-Kit信号的激活。Z近，酪氨酸激酶对生长因子信号的调控作用受到越来越多的关注，并逐渐成为一个重要的靶点[2]。

Imatinib Mesylate是一种酪氨酸激酶（Ab1、c-Kit和PDGFR）特异性YZ剂，并增加细胞对放射性ZL或化疗的敏感性。在视网膜母细胞瘤Y79和WERI-Rb-1细胞系中，Imatinib MesylateZL在10 μM的浓度下YZ细胞增殖和侵袭[3]。在成骨细胞中，给予Imatinib MesylateYZ破骨细胞发展，可能通过刺激分化、YZ增殖和存活起作用[4]。

在肥大细胞瘤的犬模型中，每天给予10 mg/kg的Imatinib Mesylate，持续1 ~ 9周，YZ酪氨酸激酶以阻碍肿瘤生长[5]。

参考文献：

[1].Buchdunger, E., et al., Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class. Proc Natl Acad Sci U S A, 1995. 92(7): p. 2558-62.

[2].Zhou, Y., et al., The multi-targeted tyrosine kinase inhibitor vandetanib plays a bifunctional role in non-small cell lung cancer cells. Sci Rep, 2015. 5: p. 8629.

[3].de Moura, L.R., et al., The effect of imatinib mesylate on the proliferation, invasive ability, and radiosensitivity of retinoblastoma cell lines. Eye (Lond), 2013. 27(1): p. 92-9.

[4].O'Sullivan, S., et al., Imatinib mesylate does not increase bone volume in vivo. Calcif Tissue Int, 2011. 88(1): p. 16-22.

[5].Isotani, M., et al., Effect of tyrosine kinase inhibition by imatinib mesylate on mast cell tumors in dogs. J Vet Intern Med, 2008. 22(4): p. 985-8