Tyrosine Kinase/Adaptateurs

Duligotuzumab (MEHD-7945A) is a bispecific humanised IgG-κ monoclonal antibody targeting HER3 and EGFR, solid tumours, head and neck cancer,colorectal cancer.

EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R/T790M/C797S and 0.06 nM for EGFR Del19/

FGFR1 inhibitor-10 (Compound 4i), with an IC50 of 28 nM, effectively inhibits FGFR1 phosphorylation.

APG-2449 is an orally active inhibitor targeting ALK, ROS1, and FAK, demonstrating antitumor efficacy in mouse models of non-small cell lung cancer (NSCLC) [1].

YK-029A, an orally active EGFR mutant inhibitor, targets both EGFR T790M and EGFRex20ins mutations.

JDB175, a selective BTK inhibitor with oral bioavailability, demonstrates excellent penetration through the blood-brain barrier.

Canlitinib, a tyrosine kinase inhibitor, holds potential for cancer research.

Syk-IN-8 (compound 19q) functions as a Syk inhibitor with demonstrated antiproliferative effects on a variety of hematological tumor cells.

TrkB-IN-1 is a potent, orally active agonist of the TrkB receptor, with favorable pharmacokinetic (PK) properties.

BTK-IN-25 (compound 71) is a potent BTK inhibitor, demonstrating an IC50 of 0.77 nM against BTK(C481S) and achieving an IC50 of 1 nM in DOHH2 cells [1].

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM.

EGFR-IN-123 (compound D06) is an effective EGFR inhibitor. It exhibits inhibitory activity against several cell lines including PC-9G, A549, A431, and HCT116, with IC50 values of 0.74, 1.36, 1.20, and 2.53 μM respectively.

EGFR-IN-122 (compound Yfq07) serves as a potent inhibitor of EGFR. It effectively inhibits the proliferation of PC-9GR and HCC827GR cells.