XMD8-87
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货号：A560552
同义名：
ACK1-B19
XMD8-87 是一种非受体酪氨酸激酶 2（TNK2）抑制剂，对 D163E 和 R806Q 突变体的 IC50 值分别为 38 nmol/L 和 113 nmol/L。
XMD8-87 化学结构
XMD8-87 3D分子结构
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XMD8-87 纯度/质量文件 产品仅供科研
货号：A560552
标准纯度：
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产品说明书
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XMD8-87 质控信息
XMD8-87 生物活性
描述
Tyrosine Kinase nonreceptor 2 (TNK2) is a cytoplasmic kinase also known as ACK1 (activated CDC42-associated kinase) which is part of a family of cytoplasmic tyrosine kinases. TNK2 mutations have been found in renal cancer cells and also in lung, ovarian, and gastric cancers[2] 50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively. XMD8-87 potently inhibits phosphorylation of TNK2 truncation mutations found in solid tumor types. But, it’s very highly cleared in vivo in rodent PK studies[3]
XMD8-87 参考文献
[1] Maxson JE, Abel ML, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Res. 2016 Jan 1;76(1):127-38.
[2] Maxson JE, Abel ML, Wang J, Deng X, Reckel S, Luty SB, Sun H, Gorenstein J, Hughes SB, Bottomly D, Wilmot B, McWeeney SK, Radich J, Hantschel O, Middleton RE, Gray NS, Druker BJ, Tyner JW. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Res. 2016 Jan 1;76(1):127-38. doi: 10.1158/0008-5472.CAN-15-0817. Epub 2015 Dec 17. PMID: 26677978; PMCID: PMC4703549.
[3] Groendyke BJ, Powell CE, Feru F, Gero TW, Li Z, Szabo H, Pang K, Feutrill J, Chen B, Li B, Gray NS, Scott DA. Benzopyrimidodiazepinone inhibitors of TNK2. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126948. doi: 10.1016/j.bmcl.2020.126948. Epub 2020 Jan 7. PMID: 31928839.
XMD8-87 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.24mL
0.45mL
0.22mL
11.22mL
2.24mL
1.12mL
22.45mL
4.49mL
2.24mL
XMD8-87 技术信息
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