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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
见说明书
- 保质期：
＞1年
- 英文名：
INK128 Free Base
- 库存：
期货2-3周
- 供应商：
上海经科化学科技有限公司
- CAS号：
1224844-38-5
- 规格：
1mg
供应商：上海经科化学科技有限公司
服务热线：400-0199-638
QQ:472482400(上海经科）
微信号：shjkchem
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本试剂(INK128)
仅供科研实验使用,不得用于其他用途！
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).
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文献和实验为头足类的乌贼，章鱼所特有的结构，是贮藏墨汁的梨形囊。墨囊只 1个，位于外套腔顶端附近正中线上，其中贮有小型墨腺的分泌物，必要时，分必物经墨管（ ink-duct）在肛门附近与从外套腔排出的水一起从漏斗排放到外界。在墨管的经路中有两处具有括约肌。
乌贼、章鱼类特有的分泌墨汁（ink， sepia）的腺体。存在于墨囊内。
Evaluation of Alterations in the Tumor Suppressor Genes INK4A and INK4B in Human Bladder Tumors
, have been subdivided into two groups on the basis of sequence homology. The first CKI family includes p21 Cip1 (4 –6 ), p27 Kip1 (7 –9 ), and p57 Kip2 (10 ,11 ). The other CKI subgroup includes four members: p16 INK4A/MTS1/CDKN2A (12 ,13 ), p15 INK4B/MTS
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