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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR

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Cat. No. Product Name Information
PC-25435

AZ14289671

EGFR inhibitor

AZ14289671 is a potent, highly selective and blood-brain barrier penetrant irreversible inhibitor of EGFR exon 20 insertion (EGFRExon20Ins) mutations, inhibits EGFR phosphorylation across EGFRExon20Ins with IC50 of 17-41 nM, spares wild-type EGFR.
PC-25021

Sevabertinib

HER2 inhibitor

Sevabertinib (BAY 2927088) is a potent, selective, reversible inhibitor of mutant epidermal growth factor receptors 2 (HER2), including HER2 exon 20 insertions and HER2 point mutations.
PC-24741

HS-10375

EGFR C797S inhibitor

HS-10375 is a potent, selective EGFR C797S tyrosine kinase inhibitor, shows potent inhibitory activity against EGFR C797S mutations (Del19/T790M/C797S, L858R/T790M/C797S, Del19/C797S, and L858R/C797S), and common and/or T790M mutations (Del19, T790M, L858R/T790M, and Del19/T790M) with IC50 < 1.5 nM.
PC-24169

Perzebertinib

HER2 inhibitor

Perzebertinib (ZN-1041, ZN-A-1041) is a potent, selective BBB penetrable HER2 tyrosine kinase inhibitor.
PC-24132

Enozertinib

EGFR inhibitor

Enozertinib (ORIC-114) is a potent, brain penetrant, orally bioavailable, irreversible inhibitor of exon 20 insertions in EGFR and HER2.
PC-24129

Emupertinib

EGFR inhibitor

Emupertinib (TAS3351) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively
PC-23725

ERBB4 agonist EF-1

ERBB4 agonist

ERBB4 agonist EF-1 is a specific small molecule ERBB4 (HER4) agonist that induce ERBB4 homodimerization with EC50 of 10.5 uM in ERBB4/ERBB4 dimerization assay, reduces cell death and hypertrophy in cardiomyocytes and decreases collagen production in cardiac fibroblasts.
PC-23314

BAY 2476568

EGFR Ex20Ins inhibitor

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.
PC-23313

TAK-285

HER2/EGFR inhibitor

TAK-285 (TAK285) is a potent, dual inhibitor of HER2 and EGFR (HER1) with IC50 of 17 nM and 23 nM, respectively.
PC-22758

MTX-531

EGFR/PI3K inhibitor

MTX-531 (MTX531) is a first-in-class, potent and selective inhibitor of EGFR and PI3K with IC50 of 15  nM and 6.4  nM (PI3Kα), respectively.
PC-22307

Mefatinib

EGFR inhibitor

Mefatinib (Mifanertinib dimaleate, MET306, MET-306) is a potent, bioavailable, second-generation, irreversible dual inhibitor of EGFR/HER2 with IC50 of 0.4/11.7 nM, respectively.
PC-21782

HSL119

HUNK inhibitor

HSL119 (HSL-119) is a potent and selective hormonally upregulated neu-associated kinase (HUNK) inhibitor, completely inhibits HUNK kinase activity at 1 uM in biochemical assays.

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