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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-BI-2865
BI-2865

Chemical Structure : BI-2865

CAS No.: 2937327-93-8

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BI-2865 (BI 2865)

货号: 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.

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2 mg ￥2180 In stock
5 mg ￥3580 In stock
10 mg ￥5580 In stock
25 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 465.58
分子式 C23H27N7O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(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

参考文献

1. Dongsung Kim, et al. Nature. 2023 May 31. doi: 10.1038/s41586-023-06123-3.

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