YN340045 AV-412 451493-31-5

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

YN340004 AEE788 497839-62-0

AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. P...

YN340294 (E/Z)-CP-724714 537705-08-1

CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.

YN340165 Icotinib 610798-31-7

Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).

YN340231 Neratinib 698387-09-6

Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-...

YN340130 Tesevatinib 781613-23-8

Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibitsEGFR,ErbB2,KDR,Flt4 and EphB4kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4nM.

YN340058 Varlitinib 845272-21-1

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.

YN340044 HKI-357 848133-17-5

HKI-357 is an irreversible dual inhibitor ofEGFR and ERBB2with IC50s of 34nM and 33nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

YN340121 Sapitinib 848942-61-0

Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold mo...

YN340035 Afatinib 850140-72-6

Afatinib (BIBW 2992) is an irreversibleEGFRfamily inhibitor with IC50s of 0.5nM, 0.4nM, 10nM and 14nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

YN340036 Afatinib dimaleate 850140-73-7

Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively 100-fold more activ...

YN340242 Gefitinib D8 857091-32-8

Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is anEGFR tyrosine kinaseinhibitor, with IC50 of 2-37nM in NR6wtEGFR cells.

YN340042 BMS-690514 859853-30-8

BMS-690514 is a potent and orally active inhibitor ofEGFR and VEGFR; hasIC50s of 5, 20 and 60nM for EGFR, HER 2 and HER 4, respectively.

YN340167 TAK-285 871026-44-7

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. Phase 1.

YN340094 BMS-599626 Hydrochloride 873837-23-1

BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailableHER1 and HER2inhibitor, with IC50s of 20 and 30nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (...

YN340199 EGFR-IN-12 879127-07-8

EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a che...

YN340062 Epertinib 908305-13-5

Epertinib (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor ofEGFR,HER2 and HER4, with IC50s of 1.48nM, 7.15nM and 2.49nM, respectively. Epertinib shows potent antitumor activity.

YN340227 NRC-2694 936446-61-6

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.

YN340190 Tucatinib 937263-43-9

Tucatinib (Irbinitinib; ARRY-380; ONT-380) is a potent and selectiveHER2inhibitor with an IC50 of 8nM.

YN340059 ARRY-380 (analog ) 937265-83-3

ARRY-380 analog, an inhibitor ofEGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.