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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-BAY 2476568
BAY 2476568

Chemical Structure : BAY 2476568

CAS No.: 2311901-93-4

BAY 2476568 (BAY-568)

货号: PC-23314Not For Human Use, Lab Use Only.

BAY 2476568 (BAY-598) is the first reversible, potent and selective inhibitor of EGFR exon 20 insertions with IC50 of 20 and 24 nM for V769_D770insASV (insASV) and D770_N771insSVD (insSVD), with a wide margin of selectivity versus WT EGFR.

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10 mg ¥4580 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

BAY 2476568 (BAY-598) is the first reversible, potent and selective inhibitor of EGFR exon 20 insertions with IC50 of 20 and 24 nM for V769_D770insASV (insASV) and D770_N771insSVD (insSVD), with a wide margin of selectivity versus WT EGFR.
BAY 2476568 (BAY-598) exhibits greater than 20-fold selectivity for EGFR exon 20 insertions compared to wild-type EGFR in isogenic Ba/F3 models and in cancer cell lines endogenously expressing EGFR exon 20 insertions.
BAY 2476568 (BAY-598) demonstrates the ability of BAY-568 to kill cancer cells harboring exon 20 insertions and other EGFR mutations with decreased activity on wild-type EGFR, irrespective of C797S mutation status.

物理化学性质&存储条件

分子量 454.50
分子式 C24H27FN4O4
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

3-[(3-Fluoro-2-methoxyphenyl)amino]-1,5,6,7-tetrahydro-2-[3-(2-methoxy-2-methylpropoxy)-4-pyridinyl]-4H-pyrrolo[3,2-c]pyridin-4-one

参考文献

1. Patent WO2019081486A1.

2. F. Siegel et al. Cancer Res. 81, 1470–1470 (2021).

3. Hanchen Zhao, et al. Proc Natl Acad Sci U S A. 2024 Nov 5;121(45):e2417144121.

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