Description
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.
Product information
CAS Number: 2031152-08-4
Molecular Weight: 536.55
Formula: C27H27F3N8O
Chemical Name: N-(3-{7-[(1,3-dimethyl-1H-pyrazol-5-yl)amino]-1-methyl-1H,2H,3H,4H-[1,3]diazino[4,5-d]pyrimidin-3-yl}-4-methylphenyl)-3-(trifluoromethyl)benzamide
Smiles: CN1CN(CC2=CN=C(NC3=CC(C)=NN3C)N=C12)C1=CC(=CC=C1C)NC(=O)C1=CC(=CC=C1)C(F)(F)F
InChiKey: MCEWMWAJAOMTBE-UHFFFAOYSA-N
InChi: InChI=1S/C27H27F3N8O/c1-16-8-9-21(32-25(39)18-6-5-7-20(11-18)27(28,29)30)12-22(16)38-14-19-13-31-26(34-24(19)36(3)15-38)33-23-10-17(2)35-37(23)4/h5-13H,14-15H2,1-4H3,(H,32,39)(H,31,33,34)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC50 of 11.4 nM. XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC50 values of 326.6 nM, 685.6 nM and 1065 nM, respectively. XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC50 of 182.3 nM against BTK(C481S)-Ba/F3 cells. XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells. XMU-MP-3 (10-1000 nM; 4 hours) inhibits both the auto- and trans-phosphorylation of BTK at the site of Y223 and Y551 in a dose-dependent manner in BTK-transformed Ba/F3 cells.
In Vivo:
XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models.
Products are for research use only. Not for human use.
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