1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Btk
    Apoptosis
  3. XMU-MP-3

XMU-MP-3 

Cat. No.: HY-136531
Handling Instructions

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.

For research use only. We do not sell to patients.

XMU-MP-3 Chemical Structure

XMU-MP-3 Chemical Structure

CAS No. : 2031152-08-4

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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[1].

IC50 & Target

IC50: 10.7 nM (BTK WT), 17.0 nM (BTK C481S), Apoptosis[1]

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[1].
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[1].
XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC50 of 182.3 nM against BTK(C481S)-Ba/F3 cells[1].
XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells[1].
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[1].

Cell Proliferation Assay[1]

Cell Line: BTK-transformed and parental Ba/F3 cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 48 hours
Result: Inhibited BTK-transformed Ba/F3 cell proliferation with an IC50 of 11.4 nM, while it showed negligible anti-proliferative effects on parental wild-type Ba/F3 cells (IC50 >10000 nM).

Western Blot Analysis[1]

Cell Line: BTK-transformed Ba/F3 cells
Concentration: 10, 50, 100, 500, 1000 nM
Incubation Time: 4 hours
Result: The phosphorylation levels of BTK Y223 and Y551 were reduced significantly at concentrations as low as 100 nM, and completely suppressed at the concentration of 1000 nM.
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.
Molecular Weight

536.55

Formula

C₂₇H₂₇F₃N₈O

CAS No.

2031152-08-4

SMILES

O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC(C)=NN4C)N=C3N(C)C2)=C1)C5=CC=CC(C(F)(F)F)=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

XMU-MP-3BtkApoptosisBruton tyrosine kinaseBtkC481SmutationmalignantB-cellsJeKo-1RamosNALM-6Inhibitorinhibitorinhibit

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