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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-BI-2852
BI-2852

Chemical Structure : BI-2852

CAS No.: 2375482-51-0

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BI-2852 (BI 2852)

货号: PC-72332Not For Human Use, Lab Use Only.

BI-2852 (BI 2852) is a potent pan-Ras inhibitor, targets GTP-bound KRAS, binds to KRASG12D with a KD of 740 nM (ITC), inhibits GTP-KRAS G12D binding to effectors like SOS1, CRAF and PI3Kα with an IC50 of 490, 770 and 500 nM.

规格 价格 库存 数量
5 mg ￥2580 In stock
10 mg ￥4380 In stock
50 mg ￥9880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BI-2852 (BI 2852) is a potent pan-Ras inhibitor, targets GTP-bound KRAS, binds to KRASG12D with a KD of 740 nM (ITC), inhibits GTP-KRAS G12D binding to effectors like SOS1, CRAF and PI3Kα with an IC50 of 490, 770 and 500 nM.
BI-2852 showed pERK(2h) modulation and antiproliferative effects in KRASmut cells (NCI-H358) at 5.8 uM and 6.7 uM, displays an IC50 of 490 nM in a GTP-KRASG12D::SOS1 AlphaScreen (AS) assay leading to low micromolar inhibition of pERK (in H358 cell line).
BI-2852 can serve as an excellent small molecule tool inhibitor of KRAS for testing biological hypotheses in vitro.

物理化学性质&存储条件

分子量 C31H28N6O2
分子式 516.605
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)-5-Hydroxy-3-(2-((((1-((1-methyl-1H-imidazol-4-yl)methyl)-1H-indol-6-yl)methyl)amino)methyl)-1H-indol-3-yl)isoindolin-1-one

参考文献

1. Kessler D, et al. Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15823-15829.

2. Tran TH, et al. Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364.

3. Kessler D, et al. Future Med Chem. 2020 Nov;12(21):1911-1923.

4. Nomura TK, et al. Cell Chem Biol. 2021 Nov 18;28(11):1581-1589.e6.

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