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CAS No.: 1234480-46-6

XMD8-87 Catalog No. CSN18846

Synonyms: ACK1-B19

XMD8-87 is a tyrosine kinase nonreceptor 2 (TNK2) inhibitor with IC50s of 38 nmol/L and 113 nmol/L for the D163E and R806Q mutations.

规格	价格	促销价格	库存	数量

400-920-2911

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tech@csnpharm.cn

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技术信息

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]. XMD8-87 is a potent TNK2 inhibitor with IC₅₀ 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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2446 mL
- 11.2229 mL
- 22.4458 mL
- 5 mM
- 0.4489 mL
- 2.2446 mL
- 4.4892 mL
- 10 mM
- 0.2245 mL
- 1.1223 mL
- 2.2446 mL

技术信息

CAS号

1234480-46-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H27N7O2

运输

蓝冰

分子量

445.52

别名

ACK1-B19

溶解度

DMSO	17.5 mg/mL (39.3 mM)
Water	insoluble

动物实验配方

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