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Background: KRAS is an important protein in the RAS/MAPK signaling pathway that transmits signals from activated cell surface receptors leading to cell proliferation and survival. KRAS function is controlled by cycling through an inactive, GDP-bound state and an active, GTP-bound state. Activation of KRAS occurs when it binds to Guanine Nucleotide Exchange Factor (GEF) proteins, including SOS, which initiate the exchange of GDP for GTP. Active, GTP-bound KRAS can trigger activation of downstream signaling molecules including RAF, PI3K, and RAL. KRAS can self-inactivate by cleaving the terminal phosphate group on the GTP, converting it to GDP. This inactivation process is accelerated by GTPase-activating (GAP) proteins.KRAS has emerged as a target of significant clinical interest, due to mutations in the KRAS protein that promote the pathogenesis of 20-30% of human cancers. Testing a patient for the presence of specific KRAS mutants serves as a highly predictive marker for success rates to various types of lung and colon cancer therapies. The development of inhibitors against KRAS G12C, G12D, and G12V holds a promising future for oncology.
CAS Number: 2937327-93-8
Description: BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM).1
Format: Solid.
Purity: ≥90%
Storage Stability: Powder, store up to 3 yeas at -20°C or up to 2 years at 4°C. In solvent, store up to 6 months at -80°C or up to 1 month at -20°C
Target: KRAS, KRAS G12C, KRAS G12D, KRAS G12V, KRAS G13D
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Kim D, et al., 2023 Nature 619: 160-166.
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