产品
编 号：F562007
分子式：C91H138N12O24
分子量：1784.14
分子式：C91H138N12O24
分子量：1784.14
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1887095-82-0
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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.
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.
体内研究：
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.
体外研究：
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.
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