Kobe2602

SKU: orb1225024

Description

kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.

Key Properties

• CAS Number: 454453-49-7
• MW: 419.31
• Purity: >98% (HPLC)
• Formula: C₁₄H₉F₄N₅O₄S
• SMILES: FC(C1=CC([N+]([O-])=O)=C(NNC(NC2=CC=C(F)C=C2)=S)C([N+]([O-])=O)=C1)(F)F
• Target: Raf
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  Kobe2602 (80 mg/kg; p.o. ; five consecutive days per week; for 17 days) exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-RasG12V gene. Animal model: Female athymic nude mice (6-8 wk old), with SW480 cells xenograft. Dosage: 80 mg/kg. Administration: Oral administration, five consecutive days per week, for 17 days. Result: Caused inhibition of the tumor growth.
• In Vitro:
  Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells. Kobe2602 has IC50 value of approximately 10 μM for the cellular Ras-Raf-binding inhibition. Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V. Kobe2602 inhibits Ras GTP but not Ras GDP. Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells. Cell Proliferation Assay Cell line: H-rasG12V-transformed NIH 3T3 cells. Concentration: 20 μM. Incubation time: 24 hours, 48 hours, 72 hours. Result: Efficiently inhibited colony formation in soft agar in a dose-dependent manner. Western blot analysis. Cell line: NIH 3T3 cells. Concentration: 2 μM, 20 μM. Incubation time: 1 hour. Result: Effectively reduced the amount of c-Raf-1 associated with H-RasG12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Kobe2602 | Kobe 2602 | Kobe-2602

Quick Database Links

Gene Symbol

Raf