Home Cell Cycle Ras inhibitor BQU57 For research use only.

BQU57

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

BQU57 Chemical Structure

BQU57 Chemical Structure

CAS No. 1637739-82-2

Purity & Quality Control

Batch: S760701 DMSO]66 mg/mL]false]Ethanol]20 mg/mL]false]Water]Insoluble]false Purity: 99.72%
99.72

BQU57 Related Products

Signaling Pathway

Ras Signaling Pathways

Ras Signaling Pathway

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 vitro In both the H2122 and H358 cell lines, BQU57 inhibits both RalA and RalB activation, and thus causes cell growth inhibition. [1]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-TBK1 30995277
In Vivo
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]
Animal Research Animal Models Mice bearing human lung H2122 tumors
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 334.1 Formula

C16H13F3N4O
CAS No. 1637739-82-2 SDF Download BQU57 SDF
Smiles CC1=NN(C2=C1C(C(=C(O2)N)C#N)C3=CC=C(C=C3)C(F)(F)F)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (197.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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