BQU57

Catalog No.S7607

BQU57 Chemical Structure

Molecular Weight(MW): 334.1

BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.

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Biological Activity

Description BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
Targets
GTPase Ral [1]
In vitro

In both the H2122 and H358 cell lines, BQU57 inhibits both RalA and RalB activation, and thus causes cell growth inhibition. [1]

Assay
Methods Test Index PMID
Western blot
p-TBK1; 

PubMed: 30995277     


HeLa cells were treated with 50 μM BQU57 for 2 hours and an Immunoblot was performed for the indicated proteins.

30995277
In vivo In mice bearing human lung H2122 tumors, BQU57 (50 mg/kg, i.p.) significantly inhibits activation of both RalA and RalB, and causes dose-dependent tumor growth inhibition. [1]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: Human lung cancer lines, H2122, H358, H460 and Calu6
  • Concentrations: ~10 μM
  • Incubation Time: 48 hours
  • Method: Growth inhibition on human lung cancer cells by the compounds are measured under anchorage-independent conditions in soft agar. Cells are seeded into 6-well plates (coated with a base layer made of 2.0 mL of 1% low-melting-point agarose) at 15,000 cells per well in 3.0 mL of 0.4% low-melting-point agarose containing various concentration of drug. Two to four weeks (depending on cell line) after incubation, cells are stained with 1.0 mg/mL Nitro Blue Tetrazolium and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in 50% reduction in colony number compared to DMSO treated control. After 48 hr, cells are subjected to the soft agar colony formation assay.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mice bearing human lung H2122 tumors
  • Formulation: DMSO
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL warmed (197.54 mM)
Ethanol 20 mg/mL warmed (59.86 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 334.1
Formula

C16H13F3N4O

CAS No. 1637739-82-2
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID