BQU57

Catalog No.S7607 Batch:S760701

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.)

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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]

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.

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.

References

[1] Yan C, et al. Nature. 2014, 515(7527), 443-447.

Selleck's BQU57 has been cited by 1 publication

RalA and RalB relocalization to depolarized mitochondria depends on clathrin-mediated endocytosis and facilitates TBK1 activation. [ PLoS One, 2019, 14(4):e0214764]	PubMed: 30995277

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.

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