S83085 |
Lys01 (trihydrochloride) |
源葉(MedMol) | ≥98% |
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- 產品描述: Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
- 靶點: IC50: 3.6 μM (1205Lu), 3.8 μM (c8161), 6 μM (LN229), 7.9 μM (HT-29);lysosomalautophagy;?Autophagy
- 體外研究:
Lys01, is a 10-fold more potent autophagy inhibitor than HCQ. Compared with HCQ, Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome. Lys01 and Lys05 produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay
- 體內研究:
With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with Lys05 76 mg/kg i.p. are observed to have arched backs and lethargy. Morphologically, EM show that cells with intact nuclear and cytoplasmic membranes contain large AVs in Lys05-treated tumors. Tumor growth is significantly impaired in Lys05-treated tumors compared with controls. Lys05 treatment results in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant three- and six-fold accumulation of AV is observed at the end of 14 d of treatment in HCQ- and Lys05-treated tumors, respectively, compared with control-treated tumors
- 參考文獻:
1. McAfee Q, et al. Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8.
- 溶解性: Soluble in DMSO、H2O
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.819 ml 9.095 ml 18.19 ml 5 mM 0.364 ml 1.819 ml 3.638 ml 10 mM 0.182 ml 0.91 ml 1.819 ml 50 mM 0.036 ml 0.182 ml 0.364 ml
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本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系,公式為:
質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)