keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RapaLink-1 is the third-generation mTOR inhibitor exploiting the unique juxtaposition of two drugs (first- and second-generation mTOR kinase inhibitors) -binding pockets to create a bivalent interaction that allows inhibition of the mutants which has resistance to the previous TORKi. The PIK3CA-AKT-mTOR pathway is one of the most commonly activated pathways in human cancers, which has led to the development of small-molecule inhibitors that target various nodes in the pathway. Two generations of mTOR inhibitors had been developed.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 5 days | $ 581.00 | |
25 mg | 5 days | $ 1,650.00 |
Description | RapaLink-1 is the third-generation mTOR inhibitor exploiting the unique juxtaposition of two drugs (first- and second-generation mTOR kinase inhibitors) -binding pockets to create a bivalent interaction that allows inhibition of the mutants which has resistance to the previous TORKi. The PIK3CA-AKT-mTOR pathway is one of the most commonly activated pathways in human cancers, which has led to the development of small-molecule inhibitors that target various nodes in the pathway. Two generations of mTOR inhibitors had been developed. |
In vitro | Rapalink-1 is more potent than first- and second-generation mTOR inhibitors. RapaLink-1 could more potently reduce levels of both p-4EBP1 and cell proliferation. Researches compared rapamycin, RapaLink-1, and MLN0128 in LN229 and U87MG. Both growth inhibition and arrest in G0/G1 were more potent in response to RapaLink-1, compared with rapamycin or MLN0128. RapaLink-1 shows potent anti-tumor efficacy in vivo. RapaLink-1 led to initial regression and subsequent stabilization of tumor size in a xenograft model, while tumors treated with vehicle, rapamycin, or MLN0128 grew steadily. |
In vivo | RapaLink-1 could durably block mTORC1. RapaLink-1 is associated with FKBP12, an abundant mTOR-interacting protein, enabling the accumulation of RapaLink-1. RapaLink-1 showed better efficacy than rapamycin or TORKi, potently blocking cancer-derived, activating mutants of mTOR. |
Molecular Weight | 1784.14 |
Formula | C91H138N12O24 |
CAS No. | 1887095-82-0 |
keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: ≥178.4 mg/mL
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Rapalink-1 1887095-82-0 Others Rapalink 1 Rapalink1 inhibitor inhibit