XL388
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
XL388是一种选择性的mTOR抑制剂,IC50值为9.9 nM[1]。
mTOR是磷脂酰肌醇3-激酶(PI3K)细胞存活途径中的成员,可监控营养物质可用性、细胞能量水平、氧水平和促有丝分裂信号,在细胞生长调控和增殖中扮演重要角色[1]。
在MCF-7细胞中,XL388可阻断p70S6K对mTORC1的磷酸化作用,IC50值为94 nM,并可阻断AKT对mTORC2的磷酸化作用,IC50值为350 nM。单独以XL388试验时,体外造血肿瘤细胞系的细胞活力被抑制。另外,XL388在基于细胞的检测中可协同加强化疗的作用,降低细胞活力[1]。
小鼠每天一次口服XL388可见其在多种异种移植模型中表现出强有力的抗肿瘤活性,尤其是在MCF-7异种移植模型中,其表现出超过100%的肿瘤生长抑制[1]。XL388在多个物种中具有很强的药代动力学性质和良好的口服暴露度。具有MCF-7异种移植肿瘤的无胸腺裸鼠口服XL388,其表现出显著的和剂量依赖的抗肿瘤活性,表明阻断mTOR信号途径是抗肿瘤活性的可能靶点[2]。
参考文献:
[1]. Nicole Miller. Abstract B146: XL388: A novel, selective, orally bioavailable mTORC1 and mTORC2 inhibitor that demonstrates pharmacodynamic and antitumor activity in multiple human cancer xenograft models. Mol Cancer Ther, 2009, 8(12 Suppl):B146.
[2]. Takeuchi CS, Kim BG, Blazey CM, 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, 56(6):2218-34.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 455.5 |
Cas No. | 1251156-08-7 |
Formula | C23H22FN3O4S |
Synonyms | XL 388;XL-388 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥6.87 mg/mL in DMSO |
Chemical Name | [7-(6-aminopyridin-3-yl)-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]-(3-fluoro-2-methyl-4-methylsulfonylphenyl)methanone |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=CC(=C1F)S(=O)(=O)C)C(=O)N2CCOC3=C(C2)C=C(C=C3)C4=CN=C(C=C4)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | XL388是一种有效的mTOR选择性抑制剂,IC50值为9.9 nM。 | |||||
靶点 | mTOR | |||||
IC50 | 9.9 nM |