1887095-82-0
Chemical Structure
RapaLink-1
- CAS No.: 1887095-82-0
- Formula:C91H138N12O24
- Molecular Weight:1784.14
InChIKey: QDOGZMBPRITPMZ-XIQIGJHASA-N
SMILES: NC1=C(C2=NC=N1)C(C3=CC=C(O4)C(N=C4N)=C3)=NN2CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCN(N=N5)C=C5COCCO[C@H](CC[C@H]6C[C@H]([C@@](CC([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H]7C)C)=O)OC)O)\C)C)=O)([H])OC([C@@](CCCC8)([H])N8C(C([C@@]9(O[C@@](C[C@@H](/C(C)=C/C=C/C=C/7)OC)([H])CC[C@H]9C)O)=O)=O)=O)C)[C@@H](C6)OC)=O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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RapaLink-1 | 99.65% | 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. | ||||||||||||||||||||
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- [1]. Fan Q, et al. A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma. Cancer Cell. 2017 Mar 13;31(3):424-435. [Content Brief]
- [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. [Content Brief]
Keywords
