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XMU-MP-3

  Cat. No.:  DC70909  
Chemical Structure
2031152-08-4
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More than 5000 active chemicals with high quality for research!
Field of application
XMU-MP-3 is a potent, selective, noncovalent BTK inhibitor with IC50 of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation.XMU-MP-3 inhibited BTK‐transformed Ba/F3 cell proliferation with an IC50 of 11.4 nM, with negligible anti‐proliferative effects on parental wild‐type Ba/F3 cells (IC50>10 uM).XMU‐MP‐3 inhibited both the autophosphorylation and trans‐phosphorylation of BTK at residues Y223 and Y551, in a dose‐dependent manner in BTK‐transformed Ba/F3 cells at concentrations as low as 100 nM and completely suppressed at 1,000 nM.XMU‐MP‐3 was considerably less potent (IC50, 2,815 nM) against proliferation of BTK(T474M)‐transformed Ba/F3 cells.XMU‐MP‐3 inhibits the growth of malignant B‐cells, inhibited phosphorylation of PLCγ2 at Y1217 and Y759, substantially suppresses tumour growth in mouse xenograft models.XMU‐MP‐3 maintained inhibitory potency with an IC50 of 182.3 nM against BTK(C481S)‐Ba/F3 cells and with an IC50 of 17.0 nM in biochemical assays, suppressed ibrutinib‐resistant BTKC481S mutation in vivo.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2031152-08-4
Chemical Name: XMU-MP-3
Formula: C27H27F3N8O
M.Wt: 536.563
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
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DC42420 Tolebrutinib Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib can be used for the research of multiple sclerosis (MS).
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DC11914 Poseltinib Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
DC8358 ONO-4059(Tirabrutinib) ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.
DC9942 GDC-0853(RG7845) GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
DC74379 DZD8586 DZD8586 is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors.
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