XMD16-5 MedChemExpress (MCE)

Product Name	XMD16-5
Synonyms	CS-2587 XMD16-5 XMD 16 5 XMD-16-5 XMD 16-5 5,11-Dihydro-2-[[4-(4-hydroxy-1-piperidinyl)phenyl]amino]-11-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one 6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one, 5,11-dihydro-2-[[4-(4-hydroxy-1-piperidinyl)phenyl]amino]-11-methyl-
CAS	1345098-78-3
EINECS
Chemical Formula	C23H24N6O2
Molecular Weight	416.48
inchi
Package	1 mg;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	XMD16-5 XMD16-5 MedChemExpress (MCE) HY-101243 1345098-78-3 98.59% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions XMD16-5 XMD16-5 MedChemExpress (MCE) HY-101243 1345098-78-3 98.59% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively. XMD16-5 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). XMD16-5 has IC50s of 16 nM and 77 nM for the D163E and R806Q mutations. The effects of XMD16-5 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 XMD16-5[1]. 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]. Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD16-5) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1]. IC50: 16 nM (TNK2, D163E mutation), 77 nM (TNK2, R806Q mutation)[1] Cellular Effect Cell Line Type Value Description 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. [Content Brief]
Last Update	2025-04-01 14:45:47

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