SMILES string
NC(S1)=C(C#N)C2=C1CCC[C@]2(C)C3=NC(C4=NC(O[C@@H](C)[C@]5([H])CCCN5C)=CC=N4)=NO3
assay
≥98% (HPLC)
form
powder
Quality Level
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Application
BI-2865 may be used for studying the Kirsten rat sarcoma virus (KRAS)signaling pathways and their role in cancer. Its selective inhibition of KRAS isused to probe the biological functions of KRAS, its mutants, and downstreamsignaling pathways to gain a deeper understanding of KRAS-related oncogenesis.
Biochem/physiol Actions
BI-2865 is a cell penetrant, selective and potent pan-KRAS inhibitor, which binds with high affinity to the inactive state of KRAS and KRAS mutants. BI-2865 blocks nucleotide exchange to prevent the activation of wild-type KRAS and a broad range of KRAS mutants. It inhibits downstream signaling and growth in cancer cells harboring mutant KRAS. It does not bind to NRAS and HRAS.
法规信息
新产品
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Antonio Tedeschi et al.
Molecular cancer therapeutics, 24(4), 550-562 (2024-12-23)
KRASG12C selective inhibitors, such as sotorasib and adagrasib, have raised hopes of targeting other KRAS-mutant alleles in patients with cancer. We report that KRAS wild-type (WT)-amplified tumor models are sensitive to treatment with the small-molecule KRAS inhibitors BI-2493 and BI-2865.
A non-covalent inhibitor with pan-KRAS potential.
Katie Kingwell
Nature reviews. Drug discovery, 22(8), 622-622 (2023-07-07)
Dongsung Kim et al.
Nature, 619(7968), 160-166 (2023-06-01)
KRAS is one of the most commonly mutated proteins in cancer, and efforts to directly inhibit its function have been continuing for decades. The most successful of these has been the development of covalent allele-specific inhibitors that trap KRAS G12C
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