OSI-027 Inhibitor CAS No. 936890-98-1

Cat. No.	Name	Size	Price
KI0852	OSI-027	5 mg	$192
	OSI-027	10 mg	$352
	OSI-027	50 mg	$1012

Chemical Characteristic

Product Name	OSI-027
CAS No.	936890-98-1
Molecular Weight	406.44
Formula	C₂₁H₂₂N₆O₃
Chemical Structure

Biological activities

OSI-027 is a potent dual inhibitor of mTORC1 and mTORC2 with IC50 values of 22 and 65 nM, respectively. OSI-027 shows more than 100-fold selectivity for mTOR relative to PI3Kα, PI3Kβ, PI3Kγ, and DNA-PK. In cell-based assays, OSI-027 inhibits mTOR signaling of phospho-4E-BP1 with an IC50 of 1 µM.^[1] OSI-027 also suppresses mRNA translation of cyclin D1 in AML cells. Moreover, OSI-027 acts as a potent suppressor of primitive leukemic precursors and is much more effective than rapamycin in eliciting antileukemic effects in vitro.^[2] OSI-027 potently inhibits proliferation of several rapamycin-sensitive and -insensitive nonengineered and engineered cancer cell lines. OSI-027 also induces cell death in tumor cell lines with activated PI3K閳ユ弬KT signaling.^[3] In a GEO colorectal xenograft models, OSI-027 (65 mg/kg) slows tumor growth more than rapamycin, consistent with inhibition of both mTORC1 and mTORC2 effectors. In H292 human lung xenograft tumors, OSI-027 treatment (50 mg/kg) has 61% median tumor growth inhibition for the duration of treatment (TGI). However, combining OSI-027 with sunitinib has a median TGI of 100% with 59% maximal tumor regression.^[1]In the COLO205 tumor model, oral OSI-027 treatment (65 mg/kg) results in 100% median TGI with 37% regression, whereas rapamycin treatment (20 mg/kg) results in 79% median TGI.^[3]

Protocols

In vitro: OSI-027 is dissolved in dimethyl sulfoxide (DMSO) at 10 mM.^[3]

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, 71(5): 1573-1583. 閵嗏偓閵嗏偓 [2] Altman JK, et al. Dual mTORC2/mTORC1 targeting results in potent suppressive effects on acute myeloid leukemia (AML) progenitors. Clin Cancer Res. 2011, 17(13): 4378-4388. 閵嗏偓閵嗏偓 [3] Bhagwat SV, et al. Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin. Mol Cancer Ther. 2011, 10(8): 1394-1406. 閵嗏偓閵嗏偓

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