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RBC8 is a specific GTPases RalA/RalB inhibitor by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases RhoA and Ras.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $40 | In Stock | In Stock | |
| 5 mg | $93 | In Stock | In Stock | |
| 10 mg | $158 | In Stock | In Stock | |
| 25 mg | $313 | In Stock | In Stock | |
| 50 mg | $496 | In Stock | In Stock | |
| 100 mg | $723 | In Stock | In Stock | |
| 200 mg | $987 | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock | In Stock |
| Description | RBC8 is a specific GTPases RalA/RalB inhibitor by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases RhoA and Ras. |
| Targets&IC50 | Ral GTPase (H358 cells):3.4 μM, GTPase (H2122 cells):3.5 μM |
| In vitro | In mice bearing H358 xenografts, RBC8 administered intraperitoneally (i.p.) at a dosage of 50 mg/kg specifically inhibits RalA and RalB, thereby suppressing tumor growth. |
| In vivo | Within living cells, RBC8k can induce a chemical shift change in RalB-GDP, thereby diminishing the activation of RalA. In Ral-dependent H2122 (IC50: 3.5 μM) and H358 (IC50: 3.4 μM) models, RBC8 leads to the inhibition of anchorage-independent growth. |
| Cell Research | 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. (Only for Reference) |
| Molecular Weight | 424.45 |
| Formula | C25H20N4O3 |
| Cas No. | 361185-42-4 |
| Smiles | COc1ccc(OC)c(c1)C1c2c(OC(N)=C1C#N)[nH]nc2-c1ccc2ccccc2c1 |
| Relative Density. | 1.40 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 42.4 mg/mL (99.89 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.71 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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