RapaLink-1

CAS No. 1887095-82-0

RapaLink-1( RapaLink 1 | RapaLink1 )

Catalog No. M12954 CAS No. 1887095-82-0

RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 523 Get Quote
25MG 1485 Get Quote
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Biological Information

  • Product Name
    RapaLink-1
  • Note
    Research use only, not for human use.
  • Brief Description
    RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors.
  • Description
    RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.
  • In Vitro
    RapaLink-1 (0-200 nM; 3 days) shows U87MG cells growth inhibition.RapaLink-1 (0-12.5 nM; 48 hours) arrests U87MG cells at G0/G1.RapaLink-1 selectively inhibits p-RPS6S235/236 and p-4EBP1T37/46 at doses as low as 1.56 nM. Rapalink-1 (100 nM; 24 to 96 hours) suppressed renal cell carcinoma (RCC) cell proliferation by inducing apoptosis and cell cycle arrest.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. :Cell Proliferation Assay Cell Line:U87MG cells Concentration:0-200 nM Incubation Time:3 days Result:Showed growth inhibition.Cell Cycle Analysis Cell Line:U87MG cells Concentration:0-12.5 nM Incubation Time:48 hours Result:Arrested cells at G0/G1.Western Blot Analysis 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. Animal Model:BALB/ Cnu/nu mice bearing U87MG intracranial xenografts 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.
  • Synonyms
    RapaLink 1 | RapaLink1
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    mTOR
  • Recptor
    mTOR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1887095-82-0
  • Formula Weight
    1784.165
  • Molecular Formula
    C91H138N12O24
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 178 mg/mL (99.77 mM)
  • SMILES
    CC1CCC2CC(C(=CC=CC=CC(CC(CC(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OCCOCC5=CN(N=N5)CCOCCOCCOCCOCCOCCOCCOCCOCCC(=O)NCCCCN6C7=NC=NC(=C7C(=N6)C8=CC9=C(C=C8)OC(=N9)N)N)C)C)O)OC)C)C)C)OC
  • Chemical Name
    40-O-(2-((1-(32-(4-amino-3-(2-aminobenzo[d]oxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-27-oxo-3,6,9,12,15,18,21,24-octaoxa-28-azadotriacontyl)-1H-1,2,3-triazol-4-yl)methoxy)ethyl)-rapamycin

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Rodrik-Outmezguine VS, et al. Nature. 2016 Jun 9;534(7606):272-6.
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