egfr tki

Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.

EGFR-TK-IN-5 (Compound NCE 2) is a thiazolyl pyrazoline derivative with significant inhibitory activity and stability against EGFR. It is applicable in tumor research.

EGFR-TK-IN-2 (compound 10b) is an EGFR-TK inhibitor with an IC50 value of 0.16 μM, and it suppresses cell proliferation.

FGF/PDGF/VEGF RTK Inhibitor is a potent, reversible, atp-competitive inhibitor against pdgfrβ, fgfr-1, and vegfr-2 (ic50 = 20, 90, and 240 nm, respectively) and effectively suppresses vegf-stimulated proliferation of hmvecs (ec50 = 420 nm).

EGFR-TK-IN-4 (compound 10k) is an effective and selective inhibitor of EGFR-TK, which possesses anti-tumor activity and can induce cellular apoptosis (Apoptosis).

EGFR-TK-IN-3 (3) acts as an inhibitor of EGFR, exhibiting an IC50 value of 2.33 μM in Erlotinib-resistant A549 cells.

BI-4732 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with high blood-brain barrier permeability, antitumor activity, inhibition of EGFR activation, and inhibition of T790M mutations.

EGFR-IN-8, a dual inhibitor targeting both EGFR and c-Met, shows potential as a promising candidate for further development in treating EGFR TKI-resistant NSCLC.

Mavelertinib (PF-06747775) is an orally available, selective and potent EGFR tyrosine kinase (EGFR TKI) inhibitor with inhibitory effects on T790M/L858R and T790M/Del, and can be used in the study of oncology and respiratory diseases.

Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective, and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). It demonstrates potent efficacy against common activating EGFR mutations and the resistant T790M mutation. Rezivertinib hydrochloride efficiently penetrates the central nervous system (CNS) and exhibits antitumor activity in conditions such as non-small cell lung cancer (NSCLC).

Transtinib is an effective and irreversible EGFR tyrosine kinase inhibitor (EGFR-TKI) that is active against L858R/T790M mutated NSCLC cell lines and xenografts.

Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively.

Dovitinib Dilactic Acid (Dovitinib (TKI-258) Dilactic Acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

Epitinib is an orally active, selective, blood-brain barrier crossing epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI).

JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1/2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.

Larotinib mesylate hydrate is a potent, broad-spectrum, and orally active tyrosine kinase inhibitor (TKI), primarily targeting EGFR with an IC50 value of 0.6 nM.

JBJ-09-063 hydrochloride is an EGFR inhibitor selective for mutants, demonstrating IC50 values of 0.147 nM, 0.063 nM, 0.083 nM, and 0.396 nM against EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S, and EGFR L747S, respectively. It effectively inhibits EGFR, Akt, and ERK1/2 phosphorylation, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and -resistant models. This compound holds potential for research on EGFR-mutant lung cancer.

EGFR-IN-23, identified as compound 8 in WO2021244502A1, is a potent EGFR tyrosine kinase inhibitor (TKI) demonstrating an inhibitory concentration (IC50) of 8.05 nM against the BaF3/EGFR-DEL19/T790M/C797S cell line.

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S mutations. It effectively reduces phosphorylation of EGFR, Akt, and ERK1/2, demonstrating efficacy in models both sensitive and resistant to EGFR tyrosine kinase inhibitors (TKI). JBJ-09-063 TFA holds potential for research in EGFR-mutant lung cancer [1].

ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor that binds to ROR1's extracellular Frizzled domain, effectively inhibiting aberrant ROR1 expression linked to non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. It modulates PI3K/AKT/mTOR signaling pathways in a ROR1-dependent manner and demonstrates potent inhibition of NSCLC cell proliferation and migration, exhibiting antitumor activity in vivo [1].

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

TAS-121 is an orally active, selective, covalent third-generation mutant EGFR tyrosine kinase inhibitor (EGFR-TKI). It effectively inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM), and Ex19del/T790M mutation (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). TAS-121 also inhibits HER2 and HER4 with an IC50 of 110 nM and 2.6 nM, respectively. This compound prevents cellular proliferation by inhibiting the phosphorylation of EGFR and its downstream signaling targets, thereby inducing apoptosis. Additionally, TAS-121 demonstrates antitumor activity in xenograft models such as SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M).