936890-98-1
936890-98-1
Chemical Structure
OSI-027
Synonym(s): ASP7486
- CAS No.: 936890-98-1
- Formula:C21H22N6O3
- Molecular Weight:406.44
IUPAC Name: (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexane-1-carboxylic acid
InChIKey: JROFGZPOBKIAEW-HAQNSBGRSA-N
SMILES: O=C([C@H]1CC[C@H](C2=NC(C(N3)=CC4=C3C(OC)=CC=C4)=C5C(N)=NC=NN52)CC1)O
Biological Activity: OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively[1][2].
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OSI-027 | 99.95% | OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively. | ||||||||||||||||||||
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OSI-027 (Standard) | ≥98% | OSI-027 (Standard) is the analytical standard of OSI-027 (HY-10423). This product is intended for research and analytical applications. OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively. | ||||||||||||||||||||
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References
- [1]. Falcon BL, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. [Content Brief]
- [2]. Mateo J, et al. A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies. Br J Cancer. 2016;114(8):889-896. [Content Brief]
Keywords
