SML4151
BI-2865
≥98% (HPLC)
别名:
(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
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
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
应用
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.
生化/生理作用
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.
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.
法规信息
新产品
此项目有
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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