XMD8-87

A selective TNK2 inhibitor

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库存: 现货

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数量
5mg

￥912.00

730.00

- +
10mg

￥1612.00

1290.00

- +
25mg

￥3250.00

2600.00

- +
50mg

￥5562.00

4450.00

- +
100mg

￥9825.00

7860.00

- +

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货号: ajci23016
CAS: 1234480-46-6
别名: ACK1-B19
分子式: C24H27N7O2
分子量: 445.52
纯度: >98%
溶解度: DMSO : ≥ 26 mg/mL (58.36 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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 the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87[1].

参考文献:
[1]. Maxson JE, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis.

Protocol

Kinase experiment:

Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD8-87) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1].

Cell experiment:

Cells are treated with the following inhibitors for 72 hours: dasatinib, AIM-100, XMD8-87 and XMD16-5. Cell viability is measured using a methanethiosulfonate (MTS)-based assay and absorbance (490 nm) is read at 1 and 3 hours after adding reagent[1].

参考文献:

[1]. Maxson JE, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis.