产品说明书

XMD8-87

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Chemical Structure| 1234480-46-6 同义名 : ACK1-B19
CAS号 : 1234480-46-6
货号 : A560552
分子式 : C24H27N7O2
纯度 : 97%
分子量 : 445.517
MDL号 : MFCD30742941
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 25 mg/mL(56.11 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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].
实验方案
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

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.