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BI-2865 is a pan-KRAS inhibitor disables oncogenic signalling and tumour growth. BI-2865 blocks nucleotide exchange to prevent the activation of wild-type KRAS and a broad range of KRAS mutants, including G12A/C/D/F/V/S, G13C/D, V14I, L19F, Q22K, D33E, Q61H, K117N and A146V/T. Inhibition of downstream signalling and proliferation was restricted to cancer cells harbouring mutant KRAS, and drug treatment suppressed KRAS mutant tumour growth in mice, without having a detrimental effect on animal weight. Most KRAS oncoproteins cycle between an active state and an inactive state in cancer cells and are dependent on nucleotide exchange for activation. Pan-KRAS inhibitors like BI-2865, have broad therapeutic implications and merit clinical investigation in patients with KRAS-driven cancers.
Product Name: BI-2865
Chemical Formula: C23H27N7O2S
Molecular Weight: 465.58
Appearance: Solid powder
Purity: > 99% by HPLC
Solubility: Soluble in DMSO
Storage: Room temperature for months, or -20ºC for 3 years
Targets: pan-KRAS; KRAS; RAS
Synonym: BI-2865; BI 2865; BI2865, RAS, KRAS
Chemical Name/IUPAC:(S)-2-amino-4-methyl-4-(3-(4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)pyrimidin- 2-yl)-1,2,4-oxadiazol-5-yl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile
SMILES Code: N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(O[C@@H][C@@H]5CCCN5C)=CC=N4)=NO3)CCC2
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