产品
编 号：F756574
分子式：C55H70N12O4S
分子量：995.29
分子式：C55H70N12O4S
分子量：995.29
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CAS No: 2882845-50-1
产品详情
生物活性：
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
体外研究：
PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFRdel19) and H1975 (EGFRL858R/T790M) with IC50s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively.PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFRdel19 degradation with a DC50 values of 0.51 nM.PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines.PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase.
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
体外研究：
PROTAC EGFR degrader 4 (compound P3) has antiproliferative activity against cancer cells A431 (EGFR WT), HCC827 (EGFRdel19) and H1975 (EGFRL858R/T790M) with IC50s of 245 ± 30 nM, 0.83 ± 0.30 nM and 203 ± 21 nM, respectively.PROTAC EGFR degrader 4 (0.3-100 nM; 48 hours) displays excellent activity of inducing EGFRdel19 degradation with a DC50 values of 0.51 nM.PROTAC EGFR degrader 4 (3 and 100 nM; 48 hours) dramatically reduces the phosphorylation of EGFR and its downstream effector Akt in HCC827 and H1975 cell lines.PROTAC EGFR degrader 4 (10 and 100 nM; 48 hours) induces 31.07% and 44.80% of HCC827 cell line to undergo apoptosis at concentration of 10 and 100 nM, respectively; and arrests both HCC827 and H1975 cell lines at G1 phase.
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