SAR245409 (XL765)
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.
SAR245409（XL765）是PI3K和mTOR的选择性双重抑制剂（对PI3Kγ的IC50值为9 nm）。
PI3K（磷脂酰肌醇-4,5-二磷酸3-激酶）是一个酶家族，参与各种细胞功能，如细胞生长、增殖、分化、运动、存活和细胞内运输，从而参与癌症的发生发展。PI3K在PI3K/Akt/mTOR通路中起着关键作用。
在PA细胞系中，联合使用XL765和TMZ可以阻止细胞生长，引起细胞凋亡[1]。在一系列携带PI3K信号传导相关突变的肿瘤细胞系中，XL765抑制PIP3在细胞膜上形成，并抑制AKT/p70S6K/S6磷酸化[2]。
在GH3细胞异种移植肿瘤小鼠模型中，联合使用XL765和TMZ抑制肿瘤生长，并减少生长激素和催乳素的血清浓度，但没有增强全身性副作用[1]。在严重联合免疫缺陷小鼠中，XL765阻止MPNST在病灶区和转移区生长[3]。在多种人类肿瘤异种移植裸鼠模型中，多次给药显著抑制肿瘤生长，这与其抗增殖和抗血管生成等作用相关[2]。
参考文献：
1. Dai C, Zhang B, Liu X et al. Inhibition of PI3K/AKT/mTOR pathway enhances temozolomide-induced cytotoxicity in pituitary adenoma cell lines in vitro and xenografted pituitary adenoma in female nude mice. Endocrinology. 2013 Mar;154(3):1247-59.
2. Yu P, Laird AD, Du X et al. Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway. Mol
Cancer Ther. 2014 May;13(5):1078-91.
3. Ghadimi MP, Lopez G, Torres KE et al. Targeting the PI3K/mTOR axis, alone and in combination with autophagy blockade, for the treatment of malignant peripheral nerve sheath tumors. Mol Cancer Ther. 2012 Aug;11(8):1758-69.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 599.66 |
| Cas No. | 1349796-36-6 |
| Formula | C31H29N5O6S |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥15 mg/mL in DMSO |
| Chemical Name | N-[4-[[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-3-methoxy-4-methylbenzamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC=C(C=C2)S(=O)(=O)NC3=NC4=CC=CC=C4N=C3NC5=CC(=CC(=C5)OC)OC)OC |
| 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 | SAR245409（XL765）是mTOR/PI3K双重抑制剂。 | |||||
| 靶点 | PI3Kγ | PI3Kα | PI3Kδ | PI3Kβ | DNA-PK | mTOR |
| IC50 | 9 nM | 39 nM | 43 nM | 113 nM | 150 nM | 157 nM |
质量控制和MSDS
- 批次:
化学结构
