|Description||Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinical trials (may be discontinued since 2008). Mubritinib(TAK 165) is a potent EGFR, HER2 and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. Mubritinib(TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib(TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.|
|Appearance||white solid powder|
|Synonyms||Mubritinib; TAK165; TAK-165; TAK-165|
|Current Developer||Takeda, Japan.|
NT113 is a pan-ERBB inhibitor with high brain penetrance. It can inhibit the growth of glioblastoma xenografts with EGFR amplification. NT113 is active against ...
AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of
Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinic...
AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-ove...
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. WZ8040 is about 30-fold more potent against EGFR T790M, ...
RG13022, a non-phenolic tyrphostin analog, is an epidermal growth factor (EGF) receptor tyrosine kinase inhibitor with potential antiproliferative effect.
Naquotinib is irreversible, third-generation, epidermal growth factor receptor (EGFR) inhibitor with IC50 value of 70 nM for NCI-H1650 cell growth. It can coval...
Mutant EGFR inhibitor
BMS-599626 Hydrochloride is a selective and efficacious orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases with potential antineoplastic ...
PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA M...
AG 555 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC50 = 0.7 μM) with 50-fold and >140-fold selectivity over ErbB2 and insulin rec...
WZ-3146 is an irreversiblely inhibitor against EGFR T790M with potential anticancer activity.
AST-1306 functions as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, res...
AG 556, a dihydroxyphen derivative, has been found to be a EGFR kinase inhibitor that could probably be effective in the study of myocardial infarct and hemodyn...
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 t...
AG 18 (10 μM) inhibits EGF-induced proliferation of GH3 cells.
BGB-283 is a selective Epidermal growth factor receptor and Proto oncogene protein b raf inhibitor under the development of BeiGene. BGB-283 shows antitumor act...
Varlitinib, also known as ARRY-543, is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. V...