XMU-MP-2
Based on 1 Customer Validation
XMU-MP-2 is a selective BRK/PTK6 inhibitor with an IC50 of 5.4 nM. XMU-MP-2 inhibits the proliferation of BRK-positive breast cancer cells and induces apoptosis. XMU-MP-2 is applicable to breast cancer-related research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.29%
- No. CAS: 2031152-10-8
- Fòrmula: C32H33F3N8O2
- Peso molecular:618.65
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
XMU-MP-2 (10-5000 nM; 4-48 h) inhibits the proliferation of BRK-transformed Ba/F3 cells with an IC50 of 29.7 nM, blocks BRK-mediated signaling pathways, and induces dose-dependent apoptosis[1].
XMU-MP-2 (50-5000 nM; 4-48 h) shows significantly reduced potency against BRKT264M-transformed Ba/F3 cells (IC50 = 340.4 nM)[1].
XMU-MP-2 (50-5000 nM; 4-48 h) potently inhibits the proliferation of BRKY447F-transformed Ba/F3 cells with an IC50 of 91.0 nM, blocks BRK-mediated signaling pathways and induces apoptosis[1].
XMU-MP-2 (50-10000 nM; 48 h) selectively inhibits the proliferation of BRK-positive breast cancer cell lines (BT-474, BT-20, MCF7, T-47D)[1].
XMU-MP-2 (0-16 μM; 0-3 days) exhibits strong synergistic antiproliferative effects with the HER2 inhibitor CP-724714 (HY-14674) in BT-474 cells, and with 4-Hydroxytamoxifen (HY-16950) in MCF7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wild-type BRK-transformed Ba/F3 cells; parental Ba/F3 cells
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Concentration:10-5000 nM (4 h for signaling inhibition); 50-5000 nM (24 h for apoptosis induction); range (48 h for antiproliferation)
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Incubation Time:4 h (signaling inhibition); 24 h (apoptosis induction); 48 h (antiproliferation)
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Result:Inhibited proliferation of wild-type BRK-transformed Ba/F3 cells with an IC50 of 29.7 nM.
Showed minimal cytotoxicity against parental Ba/F3 cells.
At 500 nM and above, dose-dependently inhibited BRK Y342 autophosphorylation, and suppressed downstream phosphorylation of STAT3 Y705, STAT5 Y694, and ERK1/2 T202/Y204 (with weaker inhibition of ERK1/2 compared to STAT3/STAT5).
Induced significant apoptosis, evidenced by cleavage of caspase-3 and PARP, and increased Annexin-V-positive cells at concentrations of 500 nM and 5000 nM.
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Cell Line:BRK-positive breast cancer cell lines BT-474, BT-20, MCF7, T-47D; BRK-negative MDA-MB-468 cells
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Concentration:/
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Incubation Time:48 h
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Result:Inhibited proliferation of BRK-positive breast cancer cells with IC50 values of 241.4 nM (BT-474), 356.4 nM (BT-20), 543.5 nM (MCF7), and 277.7 nM (T-47D).
Showed minimal antiproliferative potency against BRK-negative MDA-MB-468 cells (IC50 = 4302 nM).
Parmacokinetics
| Species | Dose | Route | T1/2 | CL | Vd |
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| Mice[1] | 1 mg/kg | i.v. | 0.9 h | 39.1 mL/min/kg | 1.7 L/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nu/nu mice (4–6 weeks old) were used to establish BRK-transformed Ba/F3 cell and BRK-positive breast cancer cell (BT-474) xenograft models[1]
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Dosage:10 mg/kg, 20 mg/kg, 40 mg/kg
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Administration:Intravenous injection, once daily for 14 consecutive days
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Result:Dose-dependently reduced tumor volume and tumor weight without obvious body weight loss or systemic toxicity.
Markedly inhibited BRKY342 autophosphorylation and downstream STAT3/STAT5/Akt/ERK1/2 signaling.
Induced apoptosis in tumor tissues as confirmed by TUNEL staining, caspase-3/PARP cleavage and Annexin-V/PI assay.
Chemical Information
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No. CAS 2031152-10-8
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Appearance Solid
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Peso molecular 618.65
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Fòrmula C32H33F3N8O2
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Color Off-white to light brown
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SMILES
O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC=C(N5CCC(O)CC5)N=C4)N=C3N(C)C2)=C1)C6=CC=CC(C(F)(F)F)=C6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (80.82 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.6164 mL | 8.0821 mL | 16.1642 mL | 40.4106 mL |
| 5 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL | 8.0821 mL | |
| 10 mM | 0.1616 mL | 0.8082 mL | 1.6164 mL | 4.0411 mL | |
| 15 mM | 0.1078 mL | 0.5388 mL | 1.0776 mL | 2.6940 mL | |
| 20 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0205 mL | |
| 25 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.6164 mL | |
| 30 mM | 0.0539 mL | 0.2694 mL | 0.5388 mL | 1.3470 mL | |
| 40 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL | |
| 50 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL | |
| 60 mM | 0.0269 mL | 0.1347 mL | 0.2694 mL | 0.6735 mL | |
| 80 mM | 0.0202 mL | 0.1010 mL | 0.2021 mL | 0.5051 mL |
XMU-MP-2 Related Classifications
HY-122664 Related Classifications
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