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RBC8

Catalog No.GC10906

Ral GTPase inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

RBC8 Chemical Structure

Cas No.: 361185-42-4

Size Price Stock Qty
5mg
$84.00
In stock
25mg
$152.00
In stock
100mg
$418.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

J82 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0–15 μM, 1h

Applications

In J82 cells overexpressing FLAG-RalA, treatment with RBC8 for 1h reduced the activation of RalA. RBC8 dose-dependently inhibited cell spreading in WT MEF cells. RBC8 treatment inhibited colony formation in H2122 and H358 cell lines with the IC50 of 3.5 μM and 3.4 μM, respectively.

Animal experiment [1]:

Animal models

H2122 and H358 human lung cancer xenograft mice models

Dosage form

Intraperitoneal injection, 50 mg/kg/d for 21 days

Application

In mice bearing H358 and H2122 xenografts, RBC8 (50 mg/kg i.p.) inhibited tumor growth via specific inhibition of RalA and RalB.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Yan C, Liu D, Li L, et al. Discovery and characterization of small molecules that target the Ral GTPase. Nature, 2014, 515(7527): 443-447.

Background

RBC8 inhibit Ral GTPase with IC50 values of 3.5 μM and 3.4 μM in Ral-dependent lines H2122 and H358 [1].

RalA and B are Ras-like GTPases. They are important drivers of metastasis and tumor growth [1].

RBC8 reduced the activation of RalA in living cells. Ral is required for spreading murine embryonic fibroblasts (MEFs) and lipid raft exocytosis on fibronectin-coated cover slips. In these cells, the spreading of WT MEFs was inhibited by the depletion of RalA via siRNA, whereas caveolin deficient (Cav1-/-) MEFs were resistant to RalA depletion. Treatment with RBC8 inhibited only the cell spreading in the WT MEFs, it did not inhibited the cell spreading in Cav1-/- MEFs. A Ral pull-down assay showed that RBC8 inhibited the activation of both RalA and RalB in both the H2122 and H358 cell lines. In H2122 and H358 cells with Ral knockdown by siRNA, treatment with RBC8 did not show further inhibition of colony formation [1].

In nude mice inoculated with H2122 human lung cancer cells subcutaneously, treatment with RBC8 at 50 mg/kg/d for 21 days (except weekends) intraperitoneally showed an inhibitory effect on tumor growth to a similar extent as dual knockdown of RalA and B. H358 is a lung cancer line. In this cell line, similar results were yielded [1].

Reference:
[1].  Yan C, Liu D, Li L, et al. Discovery and characterization of small molecules that target the Ral GTPase. Nature, 2014, 515(7527): 443-447.

Chemical Properties

Cas No. 361185-42-4 SDF
Chemical Name 6-amino-4-(2,5-dimethoxyphenyl)-3-(naphthalen-2-yl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
Canonical SMILES COC1=CC(C2C(C#N)=C(N)OC3=C2C(C4=CC=C5C(C=CC=C5)=C4)=NN3)=C(OC)C=C1
Formula C25H20N4O3 M.Wt 424.45
Solubility DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS(pH 7.2) (1:2): 0.33 mg/mL,Ethanol: 0.25 mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.356 mL 11.78 mL 23.5599 mL
5 mM 0.4712 mL 2.356 mL 4.712 mL
10 mM 0.2356 mL 1.178 mL 2.356 mL
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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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