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OSI-027

Chemical Structure : OSI-027

CAS No.: 936890-98-1

OSI-027 (OSI027;OSI 027)

Catalog No.: PC-42577Not For Human Use, Lab Use Only.

OSI-027 is a potent and selective inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

OSI-027 is a potent and selective inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.
OSI-027 displays >100-fold selectivity for mTOR over PI3Kα, PI3Kβ, PI3Kγ, and DNA-PK.
OSI-027 inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo.
OSI-027 demonstrates robust antitumor activity in human xenograft models.

Physicochemical Properties

M.Wt 406.4378
Formula C21H22N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclohexanecarboxylic acid, 4-[4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]-, trans-

References

1. Carayol N, et al. Proc Natl Acad Sci U S A. 2010 Jul 13;107(28):12469-74.

2. Falcon BL, et al. Cancer Res. 2011 Mar 1;71(5):1573-83.

3. Altman JK, et al. Clin Cancer Res. 2011 Jul 1;17(13):4378-88.

4. Bhagwat SV, et al. Mol Cancer Ther. 2011 Aug;10(8):1394-406.

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