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Chemical Structure : BI-2865
CAS No.: 2937327-93-8
Catalog No.: PC-20877Not For Human Use, Lab Use Only.
BI-2865 is a potent, inactive state selective, non-covalent pan KRAS inhibitor, binds to the GDP-loaded state of WT, G12C, G12D, G12V and G13D KRAS with high affinity (ITC Kd values,10-40 nM), inactivates common cancer-causing KRAS mutants.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $218 | In stock | |
| 5 mg | $358 | In stock | |
| 10 mg | $558 | In stock | |
| 25 mg | $898 | In stock | |
| 100 mg | Get quote |
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BI-2865 is a potent, inactive state selective, non-covalent pan KRAS inhibitor, binds to the GDP-loaded state of WT, G12C, G12D, G12V and G13D KRAS with high affinity (ITC Kd values,10-40 nM), inactivates common cancer-causing KRAS mutants.
BI-2865 inhibits the proliferation of isogenic G12C, G12D or G12V mutant KRAS expressing BaF3 cells with mean IC50 of 140 nM.
BI-2865 shows comparable activity against KRAS G12C-expressing BaF3 cells to that of covalent KRAS G12C inhibitors BI-0474 and sotorasib.
BI-2865 inhibits the activation of KRAS splice variants 4A and 4B with an IC50 of less than 10 nM, with little effect against NRAS and HRAS (IC50=5-10 uM).
BI-2865 treatment inhibited ERK and RSK phosphorylation predominantly in KRAS mutant models (mean IC50 roughly 150 nM for pERK and roughly 70 nM for pRSK), with only a small effect in WT or UAWT models.
BI-2865 suppresses MAPK output more potently in KRAS mutant models correlated, on average, with a more potent antiproliferative effect in a panel of 274 cancer cell lines.
| M.Wt | 465.58 | |
| Formula | C23H27N7O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N#CC1=C(N)SC2=C1[C@](C3=NC(C4=NC=CC(O[C@H]([C@H]5N(C)CCC5)C)=N4)=NO3)(C)CCC2 |
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1. Dongsung Kim, et al. Nature. 2023 May 31. doi: 10.1038/s41586-023-06123-3.
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