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OSI-027 Chemical Structure
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Biological Activity
OSI027 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][3]
References on OSI-027
- [] Clin Cancer Res 2011;17:4378-4388
- [] PNAS July 13, 2010;107:12469–12474
- [] Autophagy October 1, 2010;6:7, 966-967
Chemical Information
| Molecular Weight (WM): | 406.44 |
|---|---|
| Formula: | C21H22N6O3 |
| CAS No.: | 936890-98-1 |
| Synonyms: |
OSI027
|
| Dissolve in (25°C): | DMSO ≥81mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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