RBC8

Catalog No.S7606 Batch:S760601

Technical Data

Formula	C₂₅H₂₀N₄O₃
Molecular Weight	424.45	CAS No.	361185-42-4
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (197.9 mM)
		Water	Insoluble
		Ethanol	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	RBC8 is a selective inhibitor of the GTPases RalA and RalB by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases Ras and RhoA.
In vitro	In living cells, RBC8 also reduces the activation of RalA by inducing chemical shift changes in RalB–GDP. In Ral-dependent lines H2122 and H358, RBC8 causes anchorage-independent growth inhibition with IC50 of 3.5 µM and 3.4 µM, respectively. ^[1]
In vivo	In mice bearing H358 xenografts, RBC8 (50 mg/kg i.p.) inhibits tumor growth via specific inhibition of RalA and RalB. ^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Human lung cancer cell lines H2122, H358, H460 and Calu-6 Concentrations ~10 μM Incubation Time 2-4 weeks Method Growth inhibition of human lung cancer cells by the compounds is 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 the cell line) after incubation, the cells are stained with 1.0 mg ml−1 nitroblue tetrazolium, and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in a 50% reduction in colony number compared with the DMSO-treated control.
Animal Study:^{^[1]}	Animal Models Mice bearing H358 xenografts Dosages 50 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
Human lung cancer cell lines H2122, H358, H460 and Calu-6
Concentrations
~10 μM
Incubation Time
2-4 weeks
Method
Growth inhibition of human lung cancer cells by the compounds is 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 the cell line) after incubation, the cells are stained with 1.0 mg ml−1 nitroblue tetrazolium, and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in a 50% reduction in colony number compared with the DMSO-treated control.

Animal Study:^{^[1]}

Animal Models
Mice bearing H358 xenografts
Dosages
50 mg/kg
Administration
i.p.

References

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

Customer Product Validation

: Data from [Data independently produced by , , Oncotarget, 2016, 7(15): 20561-20573]

Selleck's RBC8 has been cited by 3 publications

FOXD1-dependent RalA-ANXA2-Src complex promotes CTC formation in breast cancer [ J Exp Clin Cancer Res, 2022, 41(1):301]	PubMed: 36229838
RAL GTPases mediate multiple myeloma cell survival and are activated independently of oncogenic RAS. [ Haematologica, 2019, 10.3324/haematol.2019.223024]	PubMed: 31601693
RalA, a GTPase targeted by miR-181a, promotes transformation and progression by activating the Ras-related signaling pathway in chronic myelogenous leukemia. [ Oncotarget, 2016, 7(15):20561-73]	PubMed: 26967392

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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.