XMD8-87
(Synonyms: ACK1-B19) 目录号 : GC19387
A selective TNK2 inhibitor
Cas No.:1234480-46-6
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
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]. |
References: [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. |
Cas No. | 1234480-46-6 | SDF | |
别名 | ACK1-B19 | ||
Canonical SMILES | O=C1C2=CC=CC=C2N(C)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4OC)=NC=C3N1 | ||
分子式 | C24H27N7O2 | 分子量 | 445.52 |
溶解度 | DMSO : ≥ 26 mg/mL (58.36 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 2.2446 mL | 11.2228 mL | 22.4457 mL |
5 mM | 0.4489 mL | 2.2446 mL | 4.4891 mL |
10 mM | 0.2245 mL | 1.1223 mL | 2.2446 mL |
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2.
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Quality Control & SDS
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- Purity: >98.50%
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