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RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin with MLN0128 by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.
Molecular Weight | 1784.14 |
Formula | C91H138N12O24 |
CAS Number | 1887095-82-0 |
Form | Solid |
Solubility (25°C) | DMSO 178 mg/mL (Need ultrasonic and warming) |
Storage | 4°C, dry, sealed |
[1] Kevin Lou, et al. Science. IFITM proteins assist cellular uptake of diverse linked chemotypes
[2] Ziyang Zhang, et al. Nature. Brain-restricted mTOR inhibition with binary pharmacology
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