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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-DA-0157
DA-0157

Chemical Structure : DA-0157

CAS No.: 2756978-82-0

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DA-0157 (DA0157, DAJH-1050766)

货号: PC-24040Not For Human Use, Lab Use Only.

DA-0157 (DAJH-1050766) is a potent, dual inhibitor targeting EGFR C797S mutation, ALK-positive, and EGFR/ALK co-mutations with IC50 of 6.9 nM, 5.5 nM and 7.4 nM for EGFRDel19/T790M/C797S, ALK-WT and ALK-L1196M in Ba/F3 cell assays, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DA-0157 (DAJH-1050766) is a potent, dual inhibitor targeting EGFR C797S mutation, ALK-positive, and EGFR/ALK co-mutations with IC50 of 6.9 nM, 5.5 nM and 7.4 nM for EGFRDel19/T790M/C797S, ALK-WT and ALK-L1196M in Ba/F3 cell assays, respectively.
DA-0157 shows relatively poor activity against the EGFR WT (Ba/F3-EGFR WT) with IC50 of 0.83 uM.
DA-0157 shows excellent activity against all the tested EGFR mutants (GFR (d746-750/T790 M/C797S), EGFR (T790 M/C797S/L858R), EGFR (T790 M/L792F/C797S/L858R), EGFR (T790 M/C797S), etc.) resistant to Osimertinib with IC50 between 0.10 nM and 1.69 nM, with weak IC50 against EGFRWT as 63.7 nM.
DA-0157 displays significant activity against all the tested ALK kinases including ALK WT, various point mutations and fused mutations (EML4-ALK, NPM1-ALK) with lower IC50 values (0.77 nM-1.52 nM).
DA-0157 has significant inhibitory activity against human lung cancer cells PC-9 and NCI–H1975 expressing EGFRC797S mutation (NCI-H1975, EGFRDel19/T790M/C797S, IC50=0.21 uM), but not Erlotinib and Osimertinib.
DA-0157 substantially inhibited tumor growth in the LD1-0025-200717 EGFRDel19/T790M/C797S PDX model (40 mg/kg/d, TGI: 98.3 %), Ba/F3-EML-4-ALK-L1196 M CDX model (40 mg/kg/d, TGI: 125.2 %), and NCI–H1975 EGFRDel19/T790M/C797S & NCI–H3122 (EML4-ALK) dual-side implantation CDX model (40 mg/kg/d, TGI: 89.5 % & 113.9 %).

物理化学性质&存储条件

分子量 656.61
分子式 C31H43BrN7O2P
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

(2-((5-bromo-2-((2-methoxy-5-methyl-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)-5-methylphenyl)dimethylphosphine oxide

参考文献

1. He P, et al. Eur J Med Chem. 2025 Jan 25;287:117323.

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