CAS No.: 1251156-08-7
XL388 Catalog No. CSN17119
Synonyms: XL388
XL388 is a potent and selective ATP-competitive mTOR inhibitor with IC50 value of 9.9 nM.
| 规格 | 价格 | 促销价格 | 库存 | 数量 |
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纯度 & 质量文件
批次:
靶点选择性
生物活性
- 描述
- 作用机制
动物研究 剂量 Mice: 20 mg/kg[2] (p.o.); 10 mg/kg[1] (i.v.); 50 mg/kg[3] (i.p.) Rat: 3 mg/kg[1] (i.v./p.o.) Dog: 3 mg/kg[1] (i.v./p.o.)
给药途径 p.o., i.v.
动物药代数据 Animal Mice[1] Rats[1] Dogs[1] Monkeys[1] Dose 10 mg/kg 3 mg/kg 3 mg/kg 3 mg/kg Administration i.v. or p.o. i.v. or p.o. i.v. or p.o. i.v. or p.o. F 31.4% (p.o.) 25.6% (p.o.) 69.6% (p.o.) 53.4% (p.o.) T1/2 1.35 h (i.v.) 0.45 h (i.v.) 0.45 h (i.v.) 0.86 h (i.v.) Tmax 0.5 h (p.o.) 0.5 h (p.o.) 6.11 h (p.o.) 2.0 h (p.o.) CL 2.75 L/kg/h (i.v.) 1.27 L/kg/h (i.v.) 0.598 L/kg/h (i.v.) 5.05 L/kg/h (i.v.) Cmax 9.14 μM (i.v.)
1.30 μM (p.o.)4.12 μM (i.v.)
0.707 μM (p.o.)2.28 μM (i.v.)
1.66 μM (p.o.)0.95 μM (i.v.)
0.25 μM (p.o.)AUC0→∞ 8.00 μM·h (i.v.)
2.51 μM·h (p.o.)3.72 μM·h (i.v.)
0.952 μM·h (p.o.)11.0 μM·h (i.v.)
7.66 μM·h (p.o.)1.31 μM·h (i.v.)
0.70 μM·h (p.o.)Vss 1.96 L/kg (i.v.) 1.27 L/kg (i.v.) 3.15 L/kg (i.v.) 6.42 L/kg (i.v.) - 参考文献
- [1] Takeuchi CS, Kim BG, et al. 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.
- [2] Zhu YR, Zhou XZ, et al. The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models. Oncotarget. 2016 Aug 2;7(31):49527-49538.
- [3] Yu K, Toral-Barza L, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.
- [4] 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. Epub 2013 Mar 7. PMID: 23394126.
- [5] 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; PMCID: PMC5226526.
- [6] 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; PMCID: PMC5444733.
实验方案
- 计算器
- 储存液制备
技术信息
| CAS号 | 1251156-08-7 | 储存条件 |
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| 分子式 | C23H22FN3O4S | 运输 | 蓝冰 | |||||||||
| 分子量 | 455.50 | 别名 | XL388 | |||||||||
| 溶解度 |
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动物实验配方 |
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