维基百科中的医学内容
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医学声明。
XL-388是一种药物，可用作哺乳动物雷帕霉素靶蛋白（mTOR）mTORC1和mTORC2两种亚型机制性靶标的潜在选择性抑制剂。[1]它目前处于各类癌症治疗的研究中，[2][3][4]并且mTOR抑制剂还被证明可用于神经性疼痛的治疗。[5][6]
Quick Facts 识别信息, CAS号 ...
XL-388 |
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[7-(6-aminopyridin-3-yl)-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]-(3-fluoro-2-methyl-4-methylsulfonylphenyl)methanone
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| CAS号 | 1251156-08-7 |
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| PubChem CID | |
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| CompTox Dashboard (EPA) | |
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| 化学式 | C23H22FN3O4S |
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| 摩尔质量 | 455.50 g·mol−1 |
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| 3D模型（JSmol） | |
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CC1=C(C=CC(=C1F)S(=O)(=O)C)C(=O)N2CCOC3=C(C2)C=C(C=C3)C4=CN=C(C=C4)N
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InChI=1S/C23H22FN3O4S/c1-14-18(5-7-20(22(14)24)32(2,29)30)23(28)27-9-10-31-19-6-3-15(11-17(19)13-27)16-4-8-21(25)26-12-16/h3-8,11-12H,9-10,13H2,1-2H3,(H2,25,26) Key:LNFBAYSBVQBKFR-UHFFFAOYSA-N
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Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N. Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). J Med Chem. 2013 Mar 28;56(6):2218-34. doi:10.1021/jm3007933 PMID 23394126 Zhu YR, Zhou XZ, Zhu LQ, Yao C, Fang JF, Zhou F, Deng XW, Zhang YQ. The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models. Oncotarget. 2016 Aug 2;7(31):49527-49538. doi:10.18632/oncotarget.10389 PMID 27385099 Xiong Z, Zang Y, Zhong S, Zou L, Wu Y, Liu S, Fang Z, Shen Z, Ding Q, Chen S. The preclinical assessment of XL388, a mTOR kinase inhibitor, as a promising anti-renal cell carcinoma agent. Oncotarget. 2017 May 2;8(18):30151-30161. doi:10.18632/oncotarget.15620 PMID 28404914 Zhong S, Xue J, Cao JJ, Sun B, Sun QF, Bian LG, Hu LY, Pan SJ. The therapeutic value of XL388 in human glioma cells. Aging (Albany NY). 2020 Nov 6;12(22):22550-22563. doi:10.18632/aging.103791 PMID 33159013 Choi S, Kim K, Cha M, Kim M, Lee BH. mTOR signaling intervention by Torin1 and XL388 in the insular cortex alleviates neuropathic pain. Neurosci Lett. 2020 Jan 23;718:134742. doi:10.1016/j.neulet.2020.134742 PMID 31917234 Cha M, Choi S, Kim K, Lee BH. Manganese-enhanced MRI depicts a reduction in brain responses to nociception upon mTOR inhibition in chronic pain rats. Mol Brain. 2020 Nov 23;13(1):158. doi:10.1186/s13041-020-00687-1 PMID 33267907
