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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[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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