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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

338.41

C₂₂H₁₈N₄

2097938-73-1

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 155 mg/mL (458.02 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.58 mg/mL (7.62 mM); Clear solution

  此方案可获得 ≥ 2.58 mg/mL (7.62 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: 2.58 mg/mL (7.62 mM); Clear solution; Need warming

  此方案可获得 2.58 mg/mL (7.62 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.