BQU57

Catalog No.S7607 Batch:S760701

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Technical Data

Formula

C16H13F3N4O

Molecular Weight 334.1 CAS No. 1637739-82-2
Solubility (25°C)* In vitro DMSO 66 mg/mL (197.54 mM)
Ethanol 20 mg/mL (59.86 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 (from reference)

Cell Assay:[1]
  • 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.

Animal Study:[1]
  • Animal Models

    Mice bearing human lung H2122 tumors

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Selleck's BQU57 has been cited by 2 publications

KRAS/PI3K axis driven GTF3C6 expression and promotes LUAD via FAK pathway [ J Adv Res, 2024, S2090-1232(24)00171-1] PubMed: 38685529
RalA and RalB relocalization to depolarized mitochondria depends on clathrin-mediated endocytosis and facilitates TBK1 activation. [ PLoS One, 2019, 14(4):e0214764] PubMed: 30995277

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.