BCC4004
WZ3146
WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750, EGFRE746_A750/T790M and EGFR, respectively.
BCC6667
AG 99
(E)-AG 99 ((E)-Tyrphostin 46; (E)-Tyrphostin AG 99) is a potent EGFR inhibitor.
BCN1808
Lavendustin A
Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A.
BCC5444
Mutated EGFR-IN-1
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.
BCC7667
CGP 52411
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
BCC7113
AG 825
AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity. AG825 significantly accelerates apoptosis of human neutrophils. AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development.
BCC6428
EGF816
Nazartinib (EGF816) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
BCC3974
FIIN-2
FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
BCC7434
PD 158780
PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.
BCC6436
CL-387785 (EKI-785)
CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.
BCC1418
BIBX 1382
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
BCC1666
Ixabepilone
Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
BCC1558
Erlotinib mesylate
Erlotinib mesylate (CP-358774 mesylate) inhibits purified EGFR kinase with an IC50 of 2 nM.
BCC5120
AV-412 free base
AV-412 free base (MP-412 free base) 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.
BCC5119
AV-412
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.
BCC6046
HKI 357
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
