INK128

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本试剂(INK128)
仅供科研实验使用,不得用于其他用途！

简介：
货 号：I-3344
名 称：INK128
别 名：INK128 Free Base
C A S ：1224844-38-5
分子量：309.33
分子式：C15H15N7O
纯 度：HPLC/TLC:>99%
说 明：
文 献：INK128 is a potent mTOR kinase inhibitor with a Ki of 1.4 nM. It had therapeutic benefit for prostate cancer metastasis. Hsieh A.C., et al. "The translational landscape of mTOR signalling steers cancer initiation and metastasis." Nature 485: 55-61 (2012). INK128 potently blocked cell proliferation in various breast cancer cell lines harboring PIK3CA (IC50 = 1.5-53 nM), PTEN (IC50 = 1-149 nM), KRAS and/or BRAF mutations (IC50 = 13-162 nM), and in human endothelial cells (IC50 = 33-40 nM) in vitro. In vivo, INK128 suppressed primary tumor growth significantly in both non-VEGF and VEGF-driven MCF-7 xenograft models. Gökmen-Polar Y., et al. "Investigational drug MLN0128, a novel TORC1/2 inhibitor, demonstrates potent oral antitumor activity in human breast cancer xenograft models." Breast Cancer Res. Treat. 136: 673-682 (2012). INK128 inhibited proliferation of B-cell acute lymphoblastic leukemia (B-ALL) cell lines in vitro and suppressed colony formation by primary human leukemia cells from adult and pediatric B-ALL patients. INK128 enhanced the efficacy of dasatinib in Philadelphia Chromosome-positive (Ph+) specimens. In a syngeneic mouse model of lymphoid BCR-ABL+ disease, INK128 rapidly cleared leukemic outgrowth. In non-Ph+, B-ALL xenografts, INK128 had a cytostatic effect. Janes M.R., et al. "Efficacy of the investigational mTOR kinase inhibitor MLN0128/INK128 in models of B-cell acute lymphoblastic leukemia." Leukemia 27: 586-594 (2013). The addition of lapatinib to INK-128 treatment resulted in inhibition of both PI3K/Akt/mTOR and ERK pathways and prevented both HER2 and HER3 phosphorylation induced by INK-128. This dual blockade demonstrated antitumor activity in preclinical models of breast cancer resistant to anti-HER2 therapy. García-García C., et al. "Dual mTORC1/2 and HER2 blockade results in antitumor activity in preclinical models of breast cancer resistant to anti-HER2 therapy." Clin. Cancer Res. 18: 2603-2612 (2012).