MBQ-167
MBQ-167 Basic information
- Product Name:
- MBQ-167
- Synonyms:
-
- MBQ 167;MBQ167
- MBQ-167
- 9H-Carbazole, 9-ethyl-3-(5-phenyl-1H-1,2,3-triazol-1-yl)-
- 9-Ethyl-3-(5-phenyl-1H-1,2,3-triazol-1-yl)-9H-carbazole
- Cyclin dependent kinase,MBQ-167,MBQ167,MBQ 167,Inhibitor,inhibit,CDK,Ras
- MBQ-167, 10 mM in DMSO
- MBQ-167 ，S8749
- CAS:
- 2097938-73-1
- MF:
- C22H18N4
- MW:
- 338.41
- Mol File:
- 2097938-73-1.mol
MBQ-167 Chemical Properties
- Boiling point:
- 531.8±60.0 °C(Predicted)
- Density
- 1.23±0.1 g/cm3(Predicted)
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- DMSO: Soluble
- form
- A solid
- pka
- -0.06±0.70(Predicted)
- color
- Light yellow to yellow
MBQ-167 Usage And Synthesis
Uses
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.
in vivo
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].
IC 50
Cdc42: 78 nM (IC50); Ras 1/2/3: 103 nM (IC50)
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. DOI:10.1158/1535-7163.MCT-16-0442
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