Home GPCR & G Protein Ras inhibitor RBC8 For research use only.

RBC8

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.

RBC8 Chemical Structure

RBC8 Chemical Structure

CAS No. 361185-42-4

Purity & Quality Control

Batch: S760601 DMSO]84 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.08%
99.08

RBC8 Related Products

Signaling Pathway

Ras Signaling Pathways

Ras Signaling Pathway

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 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]
Cell Research 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.
In Vivo
In vivo In mice bearing H358 xenografts, RBC8 (50 mg/kg i.p.) inhibits tumor growth via specific inhibition of RalA and RalB. [1]
Animal Research Animal Models Mice bearing H358 xenografts
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 424.45 Formula

C25H20N4O3
CAS No. 361185-42-4 SDF Download RBC8 SDF
Smiles COC1=CC(=C(C=C1)OC)C2C(=C(OC3=NNC(=C23)C4=CC5=CC=CC=C5C=C4)N)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (197.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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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