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
100MG Get Quote Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

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.
molnova catalog
related products
  • PI3Kα/mTOR-IN-1

    PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.

  • mTOR inhibitor-1

    C-4 is a potential ATP-competitive inhibitor of mTOR. C-4 could inhibit cell growth and proliferation.

  • MTI-31

    MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR).