RapaLink-1

产品信息

RapaLink-1 is the third-generation mTOR inhibitor which can overcome mTOR resistance mutations. It exploits the unique juxtaposition of two drug-binding pockets to create a bivalent interaction that allows inhibition of these resistant mutants, and reverses resistance due to mTOR FRB (resistant to Rapamycin) and kinase domain (resistant to AZD8055) mutations. RapaLink-1 is a potent mTOR inhibitor evidenced by suppression of downstream signaling, including p-AKT, p-p70S6K, p-S6 and p-4EBP1, in MCF-7 cells treated with RapaLink-1 at concentration>3nM post 4h. RapaLink-1 at low doses (3–10 nM) was the only drug regimen capable of inhibiting mTOR signalling in both F2108L mTOR- and M2327I mTOR-expressing cells. Administration of 1.5mg/kg RapaLink-1, i.p., weekly, significantly inhibited tumor growth in mice bearing RR1 or TKi-R xenograft tumors. RapaLink-1 crosses the blood-brain barrier. RapaLink-1 drove regression of intracranial brain cancers in vivo, improving survival compared with earlier-generation inhibitors, first-generation allosteric mTOR inhibitor rapamycin and second-generation TORKi.

CAS号	1887095-82-0
分子式	C91H138N12O24
主要靶点	mTOR
主要通路	PI3K/Akt/mTOR
分子量	1784.1355
MDL NO	MFCD32633594
Pubchem ID
纯度	95%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件	粉末 -20°C 3年 液体 -80°C 1年
运输条件	Shipped in cold pack
别名

靶点

Target	Activity

动物研究

剂量	Mice: 1.5 mg/kg[1] (i.p.)
给药途径	i.p.