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1887095-82-0

1887095-82-0 Structure

1887095-82-0 Structure
IdentificationBack Directory
[Name]

RapaLink-1
[CAS]

1887095-82-0
[Synonyms]

RapaLink-1
RAPALINK 1;RAPALINK1
Rapamycin, 42-O-[2-[[1-[32-[4-amino-3-(2-amino-5-benzoxazolyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-27-oxo-3,6,9,12,15,18,21,24-octaoxa-28-azadotriacont-1-yl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]-
[Molecular Formula]

C91H138N12O24
[MDL Number]

MFCD32708498
[MOL File]

1887095-82-0.mol
[Molecular Weight]

1784.17
Chemical PropertiesBack Directory
[density ]

1.30±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

≥ 178.4mg/mL in DMSO
[form ]

Solid
[pka]

10.40±0.70(Predicted)
[color ]

White to light yellow
Hazard InformationBack Directory
[Uses]

RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, 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. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity[1][2].
[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.
[IC 50]

mTOR
[References]

[1] Fan Q, et al. A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma. Cancer Cell. 2017 Mar 13;31(3):424-435. DOI:10.1016/j.ccell.2017.01.014
[2] Kuroshima K, et al. Potential new therapy of Rapalink-1, a new generation mammalian target of rapamycin inhibitor, against SU 11248-resistant renal cell carcinoma. Cancer Sci. 2020 May;111(5):1607-1618. DOI:10.1111/cas.14395
[3] Rodrik-Outmezguine VS, et al. Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor. Nature. 2016 Jun 9;534(7606):272-6. DOI:10.1038/nature17963
[4] Mu F, et al. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy both in vivo and vitro. Biochem Biophys Res Commun. 2020 Apr 30;525(2):384-391. DOI:10.1016/j.bbrc.2020.02.084
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