Product Information
Kinase Inhibitor Name R788 (Fostamatinib)
FormulaC21H22N6O3
SolubilityDMSO ≥81 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.936890-98-1
Biological ActivityOSI027 is a potent mammalian target of rapamycin (mTOR) kinase inhibitor. OSI027 has potential antineoplastic activity. MTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. MTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.
OSI027 acts as a potent suppressor of primitive leukemic precursors. OSI027 much more effective than rapamycin in eliciting antileukemic effects in vitro. OSI027 induces apoptosis of different types of cells transformed by the T315I-BCR-ABL mutation, which confers resistance to imatinib mesylate, nilotinib, and dasatinib. [1][2]
M.W.406.44
ReferencesDual mTORC2/mTORC1 Targeting Results in Potent Suppressive Effects on Acute Myeloid Leukemia (AML) Progenitors Antonella Sassano, Surinder Kaur, et al. Clin Cancer Res 2011;17:4378-4388
Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells Nathalie Carayol,Eliza Vakana,et al. PNAS July 13, 2010;107:12469–12474
Induction of autophagy by dual mTORC1-mTORC2 inhibition in BCR-ABL-expressing leukemic cells Eliza Vakana, Antonella Sassano et al. Autophagy October 1, 2010;6:7, 966-967
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction