Catalog No.
Product Name
Application
Product Information
Citations
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FGFR4 inhibitor
Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. -
BTK inhibitor
(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor. -
EGFR inhibitor
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity. -
EGFR inhibitor
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity. -
ABL inhibitor
SNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein. -
BTK inhibitor
PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively. -
FLT-3 ITD degrader
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction. -
FGFR1/DDR2 inhibitor
FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively. -
VEGFA inhibitor
PTC299 is a potent, orally bioavailable VEGFA inhibitor, targets dihydroorotate dehydrogenase (DHODH), resulting in cell growth inhibition and differentiation in leukemias, including acute myeloid leukemia, linking DHODH regulation and stress-induced VEGFA and angiogenesis. -
FAK degrader
PROTAC FAK degrader 1 is a selective and potent focal adhesion kinase (Fak) degrader with an IC50 of 6.5 nM, DC50 of 3 nM. -
ABL2 inhibitor
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively. -
HIF-PHD inhibitor
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent. - SDZ281-977 is an antiproliferative agent. It acts by binding to the ??colchicine binding site?? on tubulin and inhibiting tubulin polymerization in vitro.
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FGFR4 inhibitor
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity. -
BTK inhibitor
Poseltinib, an orally active, selective and irreversible Bruton??s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. - Epidermal Growth Factor Receptor Peptide (985-996) exists on the cell surface and is activated by the binding of its specific ligands, including epidermal growth factor and transforming growth factor.
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EGFR inhibitor
Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR. -
EGFR inhibitor
Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. -
ALK inhibitor
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase. -
ALK inhibitor
ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase. -
BTK inhibitor
AVL-292 benzenesulfonate is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM, >1400-fold selectivity over the other kinases assayed. -
Syk Inhibitor
BAY 61-3606 is a potent (Ki = 7.5 nM) and selective inhibitor of Syk kinase. -
EGFR inhibitor
Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. -
EGFR Inhibitor
Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.
