RBC8

SKU: orb1300598

Description

RBC8

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 361185-42-4
• MW: 424.45
• Purity: 99.81%
• Formula: C₂₅H₂₀N₄O₃
• SMILES: COc1ccc(OC)c(c1)C1c2c(OC(N)=C1C#N)[nH]nc2-c1ccc2ccccc2c1
• Target: GTPase,JNK,Ras,p38 MAPK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.71 mM);DMSO:42.4 mg/mL (99.89 mM)

Bioactivity

• Target IC50:
  Ral GTPase (H358 cells):3.4 μM|GTPase (H2122 cells):3.5 μM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GTPases RalA, GTPases RalB, Inhibitor, inhibit, Ras, RBC8, RBC-8, RBC 8

Compound Identifiers

PubChem CID

6626226