2. Protein Tyrosine Kinase/RTK Apoptosis Stem Cell/Wnt JAK/STAT Signaling MAPK/ERK Pathway PI3K/Akt/mTOR
  3. BRK Apoptosis STAT ERK Akt
  4. XMU-MP-2

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.

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

XMU-MP-2

XMU-MP-2 Chemical Structure

CAS No. : 2031152-10-8

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Based on 1 publication(s) in Google Scholar

XMU-MP-2 Related Antibodies

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Description

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[1].

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.

XMU-MP-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Wild-type BRK-transformed Ba/F3 cells; parental Ba/F3 cells
Concentration: 10-5000 nM (4 h for signaling inhibition); 50-5000 nM (24 h for apoptosis induction); range (48 h for antiproliferation)
Incubation Time: 4 h (signaling inhibition); 24 h (apoptosis induction); 48 h (antiproliferation)
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.

Cell Proliferation Assay[1]

Cell Line: BRK-positive breast cancer cell lines BT-474, BT-20, MCF7, T-47D; BRK-negative MDA-MB-468 cells
Concentration: /
Incubation Time: 48 h
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
Mice[1] 1 mg/kg i.v. 0.9 h 39.1 mL/min/kg 1.7 L/kg
In Vivo

XMU-MP-2 (10-40 mg/kg; intravenous injection; once daily; 14 days) significantly inhibits tumor growth and induces tumor cell apoptosis in BRK-positive breast cancer xenograft models of female BALB/c nude mice[1].

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

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]
Dosage: 10 mg/kg, 20 mg/kg, 40 mg/kg
Administration: Intravenous injection, once daily for 14 consecutive days
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.
Molecular Weight

618.65

Formula

C32H33F3N8O2
CAS No.
Appearance

Solid

Color

Off-white to light brown

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6164 mL 8.0821 mL 16.1642 mL
5 mM 0.3233 mL 1.6164 mL 3.2328 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.

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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 1.6164 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
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XMU-MP-2 Related Classifications

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  • 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-22031152-10-8BRKApoptosisSTATERKAktBreast tumor kinaseProtein tyrosine kinase 6 (PTK6)Extracellular signal regulated kinasesPKBProtein kinase Bbreast cancer cellsmouse xenograft modelsBT-474HER2 inhibitorBRK(T264M)Ba/F3 cellsPTK6ER blockadeBRK(Y447F)Inhibitorinhibitorinhibit

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