42-(Dimethylphosphinate)rapamycin
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42-(Dimethylphosphinate)rapamycin ??
- ???
- 95-98°C
- ?? ?
- 996.2±75.0 °C(Predicted)
- ??
- 1.18±0.1 g/cm3(Predicted)
- ?? ??
- Hygroscopic, -20°C Freezer, Under Inert Atmosphere
- ???
- DMSO(?? ???), ???(?? ???)
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- ?? ?? (pKa)
- 10.40±0.70(Predicted)
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- ?? ? ???? ?? (GHS)
????(GHS): |
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42-(Dimethylphosphinate)rapamycin C??? ??, ??, ??
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MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity. MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer. MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.??? ??
Off-White Solid??
ChEBI: A semisynthetic derivative that is sirolimus in which hydroxy group attached to the cyclohexyl moiety has been converted to the corresponding dimethylphosphinate.42-(Dimethylphosphinate)rapamycin ?? ?? ? ???
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42-(Dimethylphosphinate)rapamycin ?? ??
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