DDC-03-024-01

Chemical Structure : DDC-03-024-01

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货号: PC-73295Not For Human Use, Lab Use Only.

DDC-03-024-01 is a potent, mutant-selective allosteric inhibitor of EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 of 10 nM.

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生物&药学活性

DDC-03-024-01 is a potent, mutant-selective allosteric inhibitor of EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 of 10 nM.
DDC-03-024-01 displays no significant activity aginst WT EGFR (IC50>1000 nM) and high selectivity by kinome profiling.
Cotreatment with cetuximab resulted in antiproliferative activity in EGFR mutant Ba/F3 cells (IC50=0.36 uM, L858R/T790M).

物理化学性质&存储条件

分子量	508.597
分子式	C31H29FN4O2
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	10-benzyl-8-fluoro-2-(4-(4-methylpiperazin-1-yl)phenoxy)-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one

参考文献

1. Dries J H De Clercq, et al. ACS Med Chem Lett. 2019 Oct 22;10(11):1549-1553.

DDC-03-024-01

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物理化学性质&存储条件

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DDC-03-024-01

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