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EGFR

Chemical Structure Cat. No. Product Name CAS No.
BI-4020 Chemical Structure
 BCP31931 BI-4020 BI4020
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.
JBJ-04-125-02 Chemical Structure
 BCP31914 JBJ-04-125-02 2140807-05-0
JBJ-04-125-02 is a single agent can inhibit cell proliferation and EGFRL858R/T790M/C797S signaling in vitro and in vivo.
Theliatinib Chemical Structure
 BCP31409 Theliatinib 1353644-70-8
Theliatinib is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.
JND3229 Chemical Structure
 BCP31299 JND3229 JND3229
JND3229 is a new highly potent EGFRC797S reversible inhibitor with IC50 value of 5.8 nM, and also potently suppressed EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 and 6.8 nM.
Tyrphostin AG 490 Chemical Structure
 BCP21393 Tyrphostin AG 490 134036-52-5
AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
Tyrphostin A46 Chemical Structure
 BCP31172 Tyrphostin A46 122520-85-8
Tyrphostin A46 is an inhibitor of EGF receptor kinase with an IC50 value of 10 μM in the human epidermoid carcinoma cell line A431.
TAK-788 Chemical Structure
 BCP31045 TAK-788 AP32788
TAK-788 is a small, oral inhibitor of EGFR [epidermal growth factor receptor] and HER2 [human epidermal growth factor receptor 2].
Avitinib maleate Chemical Structure
 BCP19161 Avitinib maleate 1822357-78-7
Avitinib maleate, the maleate salt form of avitinib, is a pyrrolopyrimidine-based, irreversible epidermal growth factor receptor (EGFR) mutant-selective inhibitor(IC50= 7.68 nM), with potential antineoplastic activity.
Chrysophanic acid Chemical Structure
 BCP23439 Chrysophanic acid 481-74-3
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
Tesevatinib Chemical Structure
 BCP23438 Tesevatinib 781613-23-8
XL-647 (Tesevatinib, EXEL-7647, KD-019) is a novel spectrum-selective kinase inhibitor that potently inhibits the EGFR, ErbB2, KDR and EphB4 with IC50 of 0.3, 16, 1.5 and 1.4 nM, respectively.
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