Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.

BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.

AZ-5104 is a pharmacologically active metabolite derived from the demethylation of ​AZD9291 (osimertinib). It functions as a ​potent EGFR inhibitor, demonstrating strong inhibitory activity against various ​EGFR mutants and ​ErbB4.

HSL119 is a highly effective and selective inhibitor of hormonally upregulated neu-associated kinase (HUNK), demonstrating complete suppression of HUNK kinase activity at a concentration of 1 µM in biochemical assays. This compound highlights its precision and potency in targeting HUNK.

Sunvozertinib is a potent inhibitor targeting the ErbB family of receptor tyrosine kinases, including EGFR (Epidermal Growth Factor Receptor) and Her2 (Human Epidermal Growth Factor Receptor 2), as well as BTK (Bruton's Tyrosine Kinase). It exhibits particularly strong activity against mutant forms of these kinases, which are often associated with resistance to existing therapies in cancers such as non-small cell lung cancer (NSCLC). The IC50 values (half-maximal inhibitory concentr.

Allitinib (AST-1306, ALS1306)) is a novel potent, selective irreversible EGFR and HER2 inhibitor with IC50 of 0.5 and 3 nM in cell-free assays.

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.

A novel protein kinase affinity probe...

EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC).

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of

TAS2940 (TAS-2940) is a potent, selective, orally active, irreversible and brain-penetrable pan-ERBB inhibitor.

TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.

STX-721 is a potent, selective, next-generation, orally active inhibitor of EGFR exon 20 insertion mutations.

SDT-011 (SDT011) is a small molecule that effectively blocks the binding of anti-EGFR monoclonal antibodies to EGFR, blocks cetuximab-EGFR binding by 62% at 10 uM, binds to EGFR with Kd of 1.7 nM in MST assays.

MTX-241F (MTX241F) is a potent, highly selective and brain-penetrant inhibitor of EGFR, PI3K and DNA-PK with IC50 of 3 nM, 87 nM (PI3Kα) and 5.5 nM, respectively.

HNPMI is a small molecule inhibitor of epidermal growth factor receptor (EGFR) with the anticancer potential against various cancers.

HCD3514 is a novel potent, selective, fourth-generation EGFR inhibitor targeting C797S triple mutation, strongly inhibits EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S mutations with IC50 of 1.0 and 2.0 nM, respectively.

ER121 (ER-121) is a potent, dual kinase inhibitor targeting both mutant EGFR and activated erbB2 with IC50 of 0.08/0.15 nM (EGFR C797S/EGFR WT, ATP=10 uM).

BI-4732 is a potent, highly BBB penetrant, fourth-generation EGFR inhibitor against EGFR activating mutations, including C797S.

BI-1622 (BI 1622) is a potent, selective, covalent and orally active HER2 inhibitor with IC50 of 7 nM, potently inhibits HER2 exon 20 mutants while sparing WT EGFR.

A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.

An analog of ARRY-380, a potent and selective HER2 inhibitor with IC50 of 8 nM.

DZD9008 is an oral, potent, irreversible, wild type-selective EGFR TKI against EGFR or HER2 Exon20ins and other mutations.

JBJ-09-063 is a potent, mutant-selective allosteric EGFR inhibitor against EGFR L858R, T790M and C797S mutations, with IC50 of <0.1 nM for recombinant EGFR L858R/T790M kinase domain.

DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models.

RG14620 is an epidermal growth factor receptor (EGFR) inhibitor, with IC50 values of 3 μM for HER 14 colony formation and 1 pM for HER 14 DNA synthesis.

Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.