OSI-027
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.
OSI-027是一种有效的和选择性的mTORC1和mTORC2双重抑制剂，IC50值分别为22 nM和65 nM[1]。
OSI-027通过抑制mTORC1和mTORC2，被发展成为一种有效的抗癌药物。在生化实验中，OSI-027对mTOR的选择性比对其它PI3K相关激酶高100倍。在细胞实验中，OSI-027抑制mTORC1和mTORC2底物的磷酸化，包括AKT、PRAS40和S6K1，从而导致下游信号的阻断。OSI-027对mTORC1和mTORC2具有同等有效的细胞内抑制作用。在多种肿瘤细胞系中，OSI-027在抑制细胞增殖和诱导细胞死亡方面比rapamycin更有效。此外，OSI-027通过显著诱导亚G1期细胞百分比，从而引起细胞凋亡。
在MDA-MB-231乳腺癌异种移植模型和人卵巢癌异种移植模型中，OSI-027具有有效的抗肿瘤活性。OSI-027的抗肿瘤谱相当广泛，包括乳腺癌、结肠癌、肺癌、前列腺癌、淋巴瘤以及头颈癌[1]。
参考文献：
[1] Bhagwat S V, Gokhale P C, Crew A P, et al. Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin. Molecular cancer therapeutics, 2011, 10(8): 1394-1406.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 406.45 |
| Cas No. | 936890-98-1 |
| Formula | C21H22N6O3 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥32.5 mg/mL in DMSO |
| Chemical Name | (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC=CC2=C1NC(C3=C(C(N)=NC=N4)N4C([C@@H]5CC[C@@H](C(O)=O)CC5)=N3)=C2 |
| 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。 |
| 描述 | OSI-027是一种选择性的和有效的mTORC1和mTORC2双重抑制剂，IC50值分别为22 nM和65 nM。 | |||||
| 靶点 | mTORC | mTORC1 | mTORC2 | PI3Kγ | DNA-PK | |
| IC50 | 4 nM | 22 nM | 65 nM | 0.42 μM | 1.0 μM | |
质量控制和MSDS
- 批次:
化学结构
