HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23)[1].
pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities[1].
Laprituximab emtansine (IMGN-289) is an immunotoxin targeting HER1. Laprituximab emtansine is an EGFR antibody-drug conjugate (ADC) consisting of the J2898A antibody, DM1 (anti-microtubule agent) and the SMCC thioether linker. Laprituximab emtansine can be used for cancer research[1][2][3].
Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion[1].
Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Laprituximab (J2898A) is a humanized IgG1 anti-EGFR antibody that can be used for the synthesis of ADC IMGN289[1].
RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research[1].
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively[1].
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib[1][2][3][4].
VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively[1].
Lapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor with IC50s of 10.2 and 9.8 nM, respectively.
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively[1][2].
Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers[1][2][3].
EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 1.623 µM. EGFR-IN-54 shows cytotoxic activity against cancer cell lines[1].
Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively[1].
Erlotinib hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM.
Nezutatug is an anti-HER3 antibody, and used for cancer research[1].
Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
PKI-166 hydrochloride is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC50 of 0.94 µM and an EC50 of 5.3 µM[1][2].
Disitamab (RC48-0) is a humanized monoclonal antibody targeting HER2. Disitamab can be used in the synthesis of antibody-drug conjugates (ADCs), Disitamab vedotin (Disitamab vedotin (HY-P9985))[1].
Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with antitumor activity[1].
EGFR-IN-53 (Compound 7) is a potent EGFR inhibitor with an IC50 of 8.264 µM. EGFR-IN-53 shows cytotoxic activity against cancer cell lines[1].
Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[1].
EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC50 of 0.34 μM. EGFR-IN-67 shows anticancer activity[1].
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis[1].
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer[1][2].
SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC50 of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC50 of ∼20 nM). SIQ17 can be used for cancer research[1]