2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. BQU57

BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity.

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BQU57 Chemical Structure

BQU57 Chemical Structure

CAS No. : 1637739-82-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity[1][2][3].

Cellular Effect
Cell Line Type Value Description References
NCI-H2122 IC50
2.2 μM
Compound: 40
Cytotoxicity against human NCI-H2122 cells under anchorage-independent condition assessed as cell growth inhibition after 10 days by nitro blue tetrazolium-based microscopic analysis
Cytotoxicity against human NCI-H2122 cells under anchorage-independent condition assessed as cell growth inhibition after 10 days by nitro blue tetrazolium-based microscopic analysis
[PMID: 27825764]
In Vitro

BQU57 inhibits RalA/RalB activated H2122 and H358 lung cancer cell clones with IC50s of 2.0 μM (H2122) and 1.3 μM (H358), respectively[1].
BQU57 (5 μM and 10 μM; 24 h) reduces rat nucleus pulposus cell apoptosis and mitochondrial dysfunction and maintains extracellular matrix (ECM) metabolic balance by inhibiting IL-1β-induced nuclear factor κB (NF-κB) signaling pathway[2].
BQU57 (50 μM; 72 h) significantly reduces triple-negative breast cancer (TNBC) cell viability, inhibited its migration and invasion ability, and reduced non-adherent growth by blocking the RalA/RalB signaling pathway[3].

BQU57 (100 μM; 72 h) combined with Paclitaxel produced a synergistic toxic effect on TNBC cells and enhanced chemotherapy sensitivity[3].

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

BQU57 Related Antibodies

Apoptosis Analysis[2]

Cell Line: Primary rat nucleus pulposus (NP) cells
Concentration: 5 μM, 10 μM
Incubation Time: 24 h
Result: Reduced IL-1β-induced apoptosis, as indicated by decreased Annexin V-positive cells (flow cytometry) and downregulated pro-apoptotic proteins (Bax, cleaved caspase-3).
Upregulated anabolic markers (aggrecan, collagen II) and downregulated catabolic markers (MMP-3, MMP-13) in Western blot analysis, confirming ECM protection.
In Vivo

BQU57 (1 mg/kg and 5 mg/kg; ip; once a day; 6 weeks) significantly alleviated lumbar instability-induced disc degeneration in rats, reduced nucleus pulposus cell apoptosis and maintained disc structural integrity[2].
BQU57 (50 mg/kg; ip; 3 times a week; 21 days) significantly inhibited orthotopic tumor growth and lung metastasis in mice with triple-negative breast cancer (TNBC) and prolonged survival[3].

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

Animal Model: C57BL/6J mice (male, 8-week-old) with lumbar instability-induced intervertebral disc degeneration[2]
Dosage: 1 mg/kg and 5 mg/kg (dissolved in 0.9% saline)
Administration: Intraperitoneal injection daily for 6 weeks
Result: Reduced disc height loss (X-ray analysis) and histological degeneration (Safranin O-Fast Green staining).
Decreased apoptosis (TUNEL assay) and downregulated pro-inflammatory markers (MMP-13, NF-κB p65) in nucleus pulposus tissues in Immunohistochemistry assay.
Animal Model: NSG mice (female, 6-8-week-old) with orthotopic MDA-MB-231 TNBC xenografts[3]
Dosage: 50 mg/kg (dissolved in DMSO)
Administration: Intraperitoneal injection 3×/week until tumor resection criteria met (average 21 days)
Result: Significantly reduced primary tumor growth (average volume: 385 mm³ vs. 720 mm³ in controls) and spontaneous lung metastasis (75% reduction in metastatic area). Decreased RalA/B activation and NF-κB signaling in tumor tissues in WB assay.
Animal Model: FVB/N mice (female, 6-8-week-old) with MVT1 murine TNBC orthotopic tumors[3]
Dosage: 50 mg/kg (dissolved in DMSO)
Administration: Intraperitoneal injection 3×/week for 21 days
Result: Delayed tumor progression (median survival: 42 days vs. 30 days in controls) and reduced experimental lung metastasis (bioluminescence imaging).
Revealed decreased Ki67 proliferation and increased cleaved caspase-3 apoptosis in tumors in Immunohistochemistry assay.
Animal Model: NSG mice (female, 11-week-old) with TNBC patient-derived xenografts (PDX-TM00096)[3]
Dosage: 50 mg/kg (dissolved in DMSO)
Administration: Intraperitoneal injection 3×/week for 24 days
Result: Significantly inhibited PDX tumor growth (average volume: 220 mm³ vs. 550 mm³ in controls) with minimal toxicity (body weight loss <5%).
Reduced RalA/B activation and ECM degradation markers in tumor tissues.
Molecular Weight

334.30

Formula

C16H13F3N4O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=C(C#N)C(C(C(C)=NN2C)=C2O1)C3=CC=C(C(F)(F)F)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (299.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9913 mL 14.9566 mL 29.9133 mL
5 mM 0.5983 mL 2.9913 mL 5.9827 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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

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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 (7.48 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 (7.48 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9913 mL 14.9566 mL 29.9133 mL 74.7831 mL
5 mM 0.5983 mL 2.9913 mL 5.9827 mL 14.9566 mL
10 mM 0.2991 mL 1.4957 mL 2.9913 mL 7.4783 mL
15 mM 0.1994 mL 0.9971 mL 1.9942 mL 4.9855 mL
20 mM 0.1496 mL 0.7478 mL 1.4957 mL 3.7392 mL
25 mM 0.1197 mL 0.5983 mL 1.1965 mL 2.9913 mL
30 mM 0.0997 mL 0.4986 mL 0.9971 mL 2.4928 mL
40 mM 0.0748 mL 0.3739 mL 0.7478 mL 1.8696 mL
50 mM 0.0598 mL 0.2991 mL 0.5983 mL 1.4957 mL
60 mM 0.0499 mL 0.2493 mL 0.4986 mL 1.2464 mL
80 mM 0.0374 mL 0.1870 mL 0.3739 mL 0.9348 mL
100 mM 0.0299 mL 0.1496 mL 0.2991 mL 0.7478 mL
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BQU57 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:

BQU571637739-82-2BQU 57BQU-57RasInhibitorinhibitorinhibit

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