MedChemExpress - Model BI-2865 -2937327-93-8
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].MCE products for research use only. We do not sell to patients.
BI-2865
MCE China：BI-2865
Brand：MedChemExpress (MCE)
Cat. No.HY-153724
CAS：2937327-93-8
Purity：99.65%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
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).
In Vitro：BI-2865 is a derivative with a prolinol substituent and a pyrimidine linker. BI-2865 has direct ionic interaction with E62, and a water-mediated hydrogen bond network with the side chain of R68 and the main chain carbonyl of Q61, as shown in Co-crystal structures of BI-2865 bound to KRAS[1]. BI-2865 (5 days) inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells in the presence of IL-13, with a mean IC50 of roughly 140 nM[1].
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References：
[1]. Kim D, et al. Pan-KRAS inhibitor disables oncogenic signalling and tumour growth. Nature. 2023 May 31. [Content Brief]
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