MBQ-167

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MBQ-167 是 Rac/Cdc42 的双重抑制剂（在 MDA-MB-231 细胞中，IC50 分别为：Rac 1/2/3 为 103 nM，Cdc42 为 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 (≥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.

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).

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Angiogenesis

CDK

Cdc42|Ras 1/2/3

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2097938-73-1

338.41

C22H18N4

>98% (HPLC)

DMSO:155 mg/mL (458.02 mM; Need ultrasonic);H2O:< 0.1 mg/mL (insoluble)

CCN1C2=C(C3=C1C=CC=C3)C=C(N4N=NC=C4C5=CC=CC=C5)C=C2

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(-20℃)

With Ice Pack

≥ 2 years