S82876 |
CHR-6494 |
源叶(MedMol) | 98% |
- 提示:详情请下载说明书。
- 产品描述: CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer
- 靶点: haspin:2 nM (IC50);Others
- 体内研究:
CHR-6494 (50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor and cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells. CHR-6494 (20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors. CHR-6494 (20 mg/kg; intraperitoneal injection for 15 consecutive days) enhances the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo
- 参考文献:
1. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18. 2. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943. 3. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139.
- 溶解性: DMSO : 50 mg/mL (171.03 mM; Need ultrasonic)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.421 ml 17.103 ml 34.207 ml 5 mM 0.684 ml 3.421 ml 6.841 ml 10 mM 0.342 ml 1.71 ml 3.421 ml 50 mM 0.068 ml 0.342 ml 0.684 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)