MBQ-167 是一种 Rac/Cdc42 的双重抑制剂，在 MDA-MB-231 细胞中，Rac 1/2/3 和 Cdc42 的 IC50 分别为 103 nM 和 78 nM。

MBQ-167 is a dual inhibitor of Rac/Cdc42 (IC50s: 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively).

MBQ-167 causes 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. MBQ-167 (≥100 nM) causes a loss of polarity in metastatic breast cancer cells. MBQ-167(500 nM; 24 h)treatment, results in ~95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells. At earlier times (6h), MBQ-167(250 or 500 nM)treatment, induce an inhibition in Rac activity in the attached cell population, while the detached population demonstrates a ~40-50% inhibition. 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 following treatment with 250 nM MBQ-167 for 24 h .

MBQ-167 treated mice display similar doubling times for both treatments (10 and 11 days). MBQ-167-treated mice show a statistically significant reduction in tumor growth. At sacrifice, 1.0 mg/kg BW of MBQ-167 causes a ~80% reduction in tumor growth, and the 10 mg/kg BW MBQ-167 treatment results in a ~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 .

2097938-73-1

C22H18N4

338.41

DMSO:155 mg/mL (458.02 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years