Art. -Nr.: HY-136531

XMU-MP-3

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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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Reinheit: 95.78%
CAS. Nr.: 2031152-08-4
Formel: C₂₇H₂₇F₃N₈O
Molecular Weight:536.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

XMU-MP-3 Chemical Structure

CAS. Nr.: 2031152-08-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 2031152-08-4
Appearance Solid
Molecular Weight 536.55
Formel C₂₇H₂₇F₃N₈O
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8638 mL

9.3188 mL

18.6376 mL

5 mM

0.3728 mL

1.8638 mL

3.7275 mL

10 mM

0.1864 mL

0.9319 mL

1.8638 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Autoimmune Disease Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XMU-MP-3

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Autoimmune Disease Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XMU-MP-3 Related Classifications

HY-136531 Related Classifications