EGFR/HER2

AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo

OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .

XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4.

AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems.

ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.

Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.

Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor.

CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.

EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.

CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.

Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR.

D-69491 (SU11464) is a small-molecule HER2 inhibitor, which was under development for the treatment of tumours with high expression of HER2, such as breast, ovarian, lung and pancreatic carcinomas.

AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.

WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.

EGFR-IN-3 is an epidermal growth factor receptor (EGFR) inhibitor.

AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431.

DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate.

PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.

TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function.

Lazertinib (YH25448,GNS-1480) is a potent, 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, showing much higher IC50 values aganist ErbB2 and ErbB4.

Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.

Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM).

MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.

Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.

Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.

AST2818 mesylate is an EGFR inhibitor.