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Signal Inhibitors and Activators

OSI-027

$362.4/ 5mg
Quantity
Total: $362

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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.
Price362.4$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
mammalian target of rapamycin (mTOR) kinase inhibitor. MTOR kinase inhibitor OSI-027 binds to and inhibits both the and the rictor-mTOR (TOR complex 2 or TORC2) complexes of apoptosis and a decrease in tumor cell proliferation. MTOR is in some tumors and plays an important role pathway.
mammalian target of rapamycin (mTOR) kinase inhibitor. MTOR kinase inhibitor OSI-027 binds to and inhibits both the and the rictor-mTOR (TOR complex 2 or TORC2) complexes of apoptosis and a decrease in tumor cell proliferation. MTOR is in some tumors and plays an important role pathway.