CS-436;OSI-027;ASP4786;CPD2801;OSI-027, >=98%;OSI027;OSI 027;OSI-027 USP/EP/BP;OSI-027, 10 mM in DMSO;OSI-027;OSI 027;ASP4786;trans-4-[4-Amino-5-(7-methoxy-1H-i
Hygroscopic, -20°C Freezer, Under inert atmosphere
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DMSO (?? ???)
?? ?? (pKa)
4.44±0.10(Predicted)
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????(GHS):
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Warning
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P- ??
H302
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?? 4
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P264, P270, P301+P312, P330, P501
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P264
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P264
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P270
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P301+P312
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P330
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P501
...? ??? / ??? ?? ???.
NFPA 704
0
2
0
OSI-027 C??? ??, ??, ??
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The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin ) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively). It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase. OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 μM. OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.
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OSI-027 is a kinase inhibitor with anti-tumor activity, used in treatment of breast cancer.
