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Kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD. Kobe2602 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras G12V. Moreover, Kobe2602 exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras(G12V) gene by oral administration.
| Molecular Weight | 419.31 |
| Formula | C14H9F4N5O4S |
| CAS Number | 454453-49-7 |
| Solubility (25°C) | DMSO: 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ras Products |
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| BBO-8520
BBO-8520 is a first-in-class orally active covalent KRAS G12C inhibitor. BBO-8520 inhibits KRASG12C (ON) by locking the GTP-binding protein in state 1, a conformation incapable of binding effectors, thereby inhibiting the downstream signaling of KRASG12C (ON) that promotes cell proliferation. BBO-8520 also rapidly and completely blocks the RAS-RAF1 interaction, returning KRASG12C to its inactive (OFF) state. |
| RMC-9805
RMC-9805 (KRAS G12D inhibitor 18) is an orally active KRAS G12D inhibitor. RMC-9805 (KRAS G12D inhibitor 18) inhibits RAS signaling and induces apoptosis in KRAS G12D mutant cancer cells. |
| RMC-7977
RMC-7977 is a highly selective, reversible, tri-complex RAS inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS, with affinity for both mutant and wild type (WT) variants. RMC-7977 demonstrated potent activity against RAS-addicted tumours carrying various RAS genotypes, particularly against cancer models with KRAS codon 12 mutations (KRASG12X). |
| KRpep-2d
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