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MBQ-167
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MBQ-167图片
CAS NO:2097938-73-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
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25mg电议
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产品介绍
MBQ-167 (MBQ167) is a dual inhibitor of Rac/Cdc42 (Ras-related C3 botulinum toxin substrate and cell division control protein 42 homolog) with anticancer activity. It inhibits Rac 1/2/3 and Cdc42 with IC50 values of 103 nM and 78 nM in metastatic MDA-MB-231 cells, respectively. Consequently, MBQ-167 significantly decreases Rac and Cdc42 downstream effector p21-activated kinase (PAK) signaling and the activity of STAT3, without affecting Rho, MAPK, or Akt activities. MBQ-167 also inhibits breast cancer cell migration, viability, and mammosphere formation. Moreover, MBQ-167 affects cancer cells that have undergone epithelial-to-mesenchymal transition by a loss of cell polarity and inhibition of cell surface actin-based extensions to ultimately result in detachment from the substratum. Prolonged incubation (120 hours) in MBQ-167 decreases metastatic cancer cell viability with a GI50 of approximately 130 nmol/L, without affecting noncancer mammary epithelial cells. The loss in cancer cell viability is due to MBQ-167-mediated G2-M cell-cycle arrest and subsequent apoptosis, especially of the detached cells. In vivo, MBQ-167 inhibits mammary tumor growth and metastasis in immunocompromised mice by approximately 90%. In conclusion, MBQ-167 is 10× more potent than other currently available Rac/Cdc42 inhibitors and has the potential to be developed as an anticancer drug, as well as a dual inhibitory probe for the study of Rac and Cdc42.
理化性质和储存条件
Molecular Weight (MW) 338.41
Formula C22H18N4
CAS No. 2097938-73-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>155 mg/mL
Water: <1 mg/mL
Ethanol:>10 mg/mL
Chemical Name 9-ethyl-3-(5-phenyl-1H-1,2,3-triazol-1-yl)-9H-carbazole
Synonyms MBQ-167; MBQ167; MBQ 167
实验参考方法
In Vitro

In vitro activity: MBQ-167 is a dual inhibitor of Rac/Cdc42 (Ras-related C3 botulinum toxin substrate and cell division control protein 42 homolog), with IC50 values of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in metastatic MDA-MB-231 cells, respectively. Consequently, MBQ-167 significantly decreases Rac and Cdc42 downstream effector p21-activated kinase (PAK) signaling and the activity of STAT3, without affecting Rho, MAPK, or Akt activities. MBQ-167 also inhibits breast cancer cell migration, viability, and mammosphere formation. Moreover, MBQ-167 affects cancer cells that have undergone epithelial-to-mesenchymal transition by a loss of cell polarity and inhibition of cell surface actin-based extensions to ultimately result in detachment from the substratum. Prolonged incubation (120 hours) in MBQ-167 decreases metastatic cancer cell viability with a GI50 of approximately 130 nmol/L, without affecting noncancer mammary epithelial cells. The loss in cancer cell viability is due to MBQ-167-mediated G2-M cell-cycle arrest and subsequent apoptosis, especially of the detached cells. In vivo, MBQ-167 inhibits mammary tumor growth and metastasis in immunocompromised mice by approximately 90%. In conclusion, MBQ-167 is 10× more potent than other currently available Rac/Cdc42 inhibitors and has the potential to be developed as an anticancer drug, as well as a dual inhibitory probe for the study of Rac and Cdc42.


Kinase Assay: MBQ-167 is a dual inhibitor of Rac/Cdc42 (Ras-related C3 botulinum toxin substrate and cell division control protein 42 homolog), with IC50 values of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in metastatic MDA-MB-231 cells, respectively.


Cell Assay: MDA-MB-231 cells are treated with vehicle or MBQ-167 at 250 or 500 nM for 24 h. Cells are fixed, permeabilized, and stained with Rhodamine phalloidin to visualize F-actin, and with p-tyrosine or vinculin to visualize focal adhesions.

In VivoMBQ-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).
Animal model Female athymic nu/nu mice, 4 to 5wk old
Formulation & Dosage Dissolved in 12.5% ethanol, 12.5% Cremophor and 75% 1X PBS pH 7.4; 1 or 10 mg/kg; i.p.
References Mol Cancer Ther. 2017 May;16(5):805-818.