1. PI3K/Akt/mTOR
    Autophagy
  2. mTOR
    Autophagy
  3. RapaLink-1

RapaLink-1 

Cat. No.: HY-111373
Handling Instructions

RapaLink-1 is the third-generation bivalent mTOR inhibitor that combines Rapamycin with MLN0128 (a second-generation mTOR kinase inhibitor) 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. Anticancer activity.

For research use only. We do not sell to patients.

RapaLink-1 Chemical Structure

RapaLink-1 Chemical Structure

CAS No. : 1887095-82-0

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Description

RapaLink-1 is the third-generation bivalent mTOR inhibitor that combines Rapamycin with MLN0128 (a second-generation mTOR kinase inhibitor) 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. Anticancer activity[1][2].

In Vitro

RapaLink-1 (0-200 nM; 3 days) shows U87MG cells growth inhibition[1].
RapaLink-1 (0-12.5 nM; 48 hours) arrests U87MG cells at G0/G1[1].
RapaLink-1 selectively inhibits p-RPS6S235/236 and p-4EBP1T37/46 at doses as low as 1.56 nM[1].
RapaLink-1 exploits the unique juxtaposition of two drug-binding pockets to create a bivalent interaction. RapaLink-1 overcomes resistance to existing first- and second-generation inhibitors[3].

Cell Proliferation Assay[1]

Cell Line: U87MG cells
Concentration: 0-200 nM
Incubation Time: 3 days
Result: Showed growth inhibition.

Cell Cycle Analysis[1]

Cell Line: U87MG cells
Concentration: 0-12.5 nM
Incubation Time: 48 hours
Result: Arrested cells at G0/G1.

Western Blot Analysis[1]

Cell Line: U87MG cells
Concentration: 0.39-12.5 nM
Incubation Time: 3 hours
Result: Selectively inhibited p-RPS6S235/236 and p-4EBP1T37/46 at doses as low as 1.56 nM. The mTORC2 targets p-AKTS473, p-SGK1S78, and p-NDRG1T346, and the p-AKTS473 target p-GSK3βS9 was inhibited only at high doses.
In Vivo

RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy[1].

Animal Model: BALB/ Cnu/nu mice bearing U87MG intracranial xenografts[1]
Dosage: 1.5 mg/kg
Administration: I.p.; every 5 days for 25 days, then once a week for 11 week
Result: Led to initial regression and subsequent stabilization of tumor size.
Molecular Weight

1784.14

Formula

C₉₁H₁₃₈N₁₂O₂₄

CAS No.

1887095-82-0

SMILES

NC1=C(C2=NC=N1)C(C3=CC=C(O4)C(N=C4N)=C3)=NN2CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCN(N=N5)C=C5COCCO[[email protected]](CC[[email protected]]6C[[email protected]]([[email protected]@](CC([[email protected]@H](/C=C([[email protected]]([[email protected]](C([[email protected]@H](C[[email protected]@H]7C)C)=O)OC)O)\C)C)=O)([H])OC([[email protected]@](CCCC8)([H])N8C(C([[email protected]@]9(O[[email protected]@](C[[email protected]@H](/C(C)=C/C=C/C=C/7)OC)([H])CC[[email protected]]9C)O)=O)=O)=O)C)[[email protected]@H](C6)OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

RapaLink-1RapaLink1RapaLink 1mTORAutophagyMammalian target of Rapamycinresistancemutationthird-generationblood-brainbarrieranticancerbivalentregressionInhibitorinhibitorinhibit

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