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Merck
CN

SML4151

BI-2865

new

≥98% (HPLC)

Synonym(s):

(4S)-2-Amino-4,5,6,7-tetrahydro-4-methyl-4-[3-[4-[(1S)-1-[(2S)-1-methyl-2-pyrrolidinyl]ethoxy]-2-pyrimidinyl]-1,2,4-oxadiazol-5-yl]- benzo[b]thiophene-3-carbonitrile, (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

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About This Item

Empirical Formula (Hill Notation):
C23H27N7O2S
CAS Number:
2937327-93-8
Molecular Weight:
465.57
MDL number:
MFCD35067897

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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

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 is used to probe the biological functions of KRAS, its mutants, and downstream signaling pathways to gain a deeper understanding of KRAS-related oncogenesis.

Biochem/physiol Actions

Cell penetrant, selective and potent pan-KRAS inhibitor, which binds with high affinity to the inactive state of KRAS and KRAS mutants.
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.

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000465279
0000465274
0000465274
0000465279
0000451030

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A non-covalent inhibitor with pan-KRAS potential.
Katie Kingwell
Nature reviews. Drug discovery, 22(8), 622-622 (2023-07-07)
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.
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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