| Identification | Back Directory | [Name]
Benzamide, N-[3-[7-[(1,3-dimethyl-1H-pyrazol-5-yl)amino]-1,4-dihydro-1-methylpyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)- | [CAS]
2031152-08-4 | [Synonyms]
XMU-MP-3
Benzamide, N-[3-[7-[(1,3-dimethyl-1H-pyrazol-5-yl)amino]-1,4-dihydro-1-methylpyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)- | [Molecular Formula]
C27H27F3N8O | [MOL File]
2031152-08-4.mol | [Molecular Weight]
536.55 |
| Hazard Information | Back Directory | [Uses]
XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis[1]. | [in vivo]
XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models[1]. | Animal Model: | Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models[1] | | Dosage: | 25 and 50 mg/kg | | Administration: | Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days | | Result: | Significantly reduced the tumor size without affecting animal weights. |
| [References]
[1] Fu Gui, et al. A Non-Covalent Inhibitor XMU-MP-3 Overrides Ibrutinib-Resistant Btk C481S Mutation in B-cell Malignancies. Br J Pharmacol. 2019 Dec;176(23):4491-4509. DOI:10.1111/bph.14809 |
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