MBQ-167 |
Catalog No.GC32970
One-Click Copy Product Info
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MBQ-167 es un inhibidor dual Rac/Cdc42, con IC50 de 103 nM para Rac 1/2/3 y 78 nM para Cdc42 en células MDA-MB-231, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2097938-73-1
Sample solution is provided at 25 µL, 10mM.
MBQ-167 is a dual Rac/Cdc42 inhibitor, with IC50s of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively.
MBQ-167 (≥100 nM) induces a loss of polarity in metastatic breast cancer cells. Treatment with 500 nM MBQ-167 for 24 h results in ~95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells. Moreover, MBQ-167 induces this phenotype in multiple mesenchymal cancer cell types including GFP-HER2-BM, MDA-MB-468, and Hs578t human breast cancer cells, as well as Mia-PaCa-2 pancreatic cancer cells, SKOV3 ovarian cancer cells, AGS and NCI-N87 gastric cancer cells, and SH-SY5Y neuroblastoma cells. Following treatment with 250 nM MBQ-167 for 24 h, the attached population of MDA-MB-231 cells demonstrate a ~25% decrease in Rac activation while the detached cells are more responsive with a ~75% decrease. At earlier times (6h), treatment with 250 or 500 nM MBQ-167, induce a inhibition in Rac activity in the attached cell population, while the detached population demonstrate a ~40-50% inhibition[1].
MBQ-167-treated mice demonstrate a statistically significant reduction in tumor growth. At sacrifice, 1.0 mg/kg BW of MBQ-167 results in a ~80% reduction in tumor growth, and the 10 mg/kg BW MBQ-167 treatment results in ~95% reduction in tumor growth. Since EHop-016 only exerts ~40% reduction of tumor growth at 10 mg/kg BW, MBQ-167 is 10X more effective than EHop-016. MBQ-167 treated mice demonstrate similar doubling times for both treatments (10 and 11 days)[1].
[1]. Humphries-Bickley T, et al. Characterization of a Dual Rac/Cdc42 Inhibitor MBQ-167 in Metastatic Cancer. Mol Cancer Ther. 2017 May;16(5):805-818.
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Animal experiment: |
Mice[1]Female athymic nu/nu mice, 4 to 5wk old are used. GFP-HER2-BM cells (~5×105) in Matrigel are injected at the fourth right mammary fat pad under isofluorane inhalation to produce orthotopic primary tumors. After tumor establishment (1wk post-inoculation), animals are randomly divided into treatment groups (n=6). Mice are treated with vehicle (12.5% ethanol, 12.5% Cremophor, and 75% 1X PBS pH 7.4), or 1 or 10 mg/kg BW MBQ-167 by i.p. injection in a 100 μL volume 3X a wk. Treatments continue until sacrifice at day 65[1]. |
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References: [1]. Humphries-Bickley T, et al. Characterization of a Dual Rac/Cdc42 Inhibitor MBQ-167 in Metastatic Cancer. Mol Cancer Ther. 2017 May;16(5):805-818. |
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| Cas No. | 2097938-73-1 | SDF | |
| Canonical SMILES | CCN1C2=C(C3=C1C=CC=C3)C=C(N4N=NC=C4C5=CC=CC=C5)C=C2 | ||
| Formula | C22H18N4 | M.Wt | 338.41 |
| Solubility | DMSO : 155 mg/mL (458.02 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.955 mL | 14.775 mL | 29.55 mL |
| 5 mM | 591 μL | 2.955 mL | 5.91 mL |
| 10 mM | 295.5 μL | 1.4775 mL | 2.955 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)