RapaLink-1,1887095-82-0

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RapaLink-1

CAS No. : 1887095-82-0

MCE 国际站：RapaLink-1

产品活性：RapaLink-1 是第三代 mTOR 抑制剂，通过 linker 将雷帕霉素 (Rapamycin, HY-10219) 与二代 mTOR 抑制剂 MLN0128 (HY-13328) 结合。RapaLink-1 比雷帕霉素或 mTOR 抑制剂 (TORKi) 更有效，能有效地阻断癌源性的，激活的 mTOR 突变体。RapaLink-1 可以穿过血脑屏障。RapaLink-1 与 FKBP12 的结合导致持久抑制 mTORC1。RapaLink-1 通过促进自噬在抗磷脂综合征中发挥抗血栓作用。具有抗癌活性。

研究领域：PI3K/Akt/mTOR  |  Autophagy

作用靶点：mTOR  |  Autophagy

In Vitro: 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-RPS6^S235/236 and p-4EBP1^T37/46 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.

In Vivo: RapaLink-1 (i.p.; every 5 days for 25 days, then once a week for 11 week) shows potent anti-tumor efficacy.

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