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OSI-027

$110$900

Products Details

Product Description

– 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].

Web ID

– HY-10423

Storage Temperature

– -20°C, 3 years (Powder)

Shipping

– Blue Ice

Applications

– Cancer-Kinase/protease

Molecular Formula

– C21H22N6O3

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.|[2]Zhi X, et al. OSI-027 modulates acute graft-versus-host disease after liver transplantation in a rat model. Liver Transpl. 2017 Sep;23(9):1186-1198.|[3]Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56.|[4]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.

CAS Number

– 936890-98-1

Molecular Weight

– 406.44

Compound Purity

– 99.40

SMILES

– O=C([C@H]1CC[C@H](C2=NC(C(N3)=CC4=C3C(OC)=CC=C4)=C5C(N)=NC=NN52)CC1)O

Clinical Information

– Phase 1

Research Area

– Cancer

Solubility

– DMSO : 125 mg/mL (ultrasonic)

Target

– Autophagy;mTOR

Isoform

– mTOR;mTORC1;mTORC2

Pathway

– Autophagy;PI3K/Akt/mTOR

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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