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

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.

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XMU-MP-3 Chemical Structure

XMU-MP-3 Chemical Structure

CAS No. : 2031152-08-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
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10 mg USD 780 In-stock
50 mg USD 2300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

XMU-MP-3 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

XMU-MP-3 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Light yellow to brown

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (186.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8638 mL 9.3188 mL 18.6376 mL
5 mM 0.3728 mL 1.8638 mL 3.7275 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8638 mL 9.3188 mL 18.6376 mL 46.5940 mL
5 mM 0.3728 mL 1.8638 mL 3.7275 mL 9.3188 mL
10 mM 0.1864 mL 0.9319 mL 1.8638 mL 4.6594 mL
15 mM 0.1243 mL 0.6213 mL 1.2425 mL 3.1063 mL
20 mM 0.0932 mL 0.4659 mL 0.9319 mL 2.3297 mL
25 mM 0.0746 mL 0.3728 mL 0.7455 mL 1.8638 mL
30 mM 0.0621 mL 0.3106 mL 0.6213 mL 1.5531 mL
40 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
50 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9319 mL
60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7766 mL
80 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5824 mL
100 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4659 mL
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XMU-MP-3 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XMU-MP-32031152-08-4BtkApoptosisBruton tyrosine kinaseBtkC481SmutationmalignantB-cellsJeKo-1RamosNALM-6Inhibitorinhibitorinhibit

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