EGFR

EGFR

The receptor tyrosine kinase family of the epidermal growth factor, which also includes HER2/neu (ErbB2), ErbB3 (HER3), and ErbB4 (HER4), includes the epidermal growth factor receptor (EGFR; ErbB1). The extracellular ligand-binding ectodomain, the single chain transmembrane domain, and the intracellular tyrosine kinase domain make up the EGFR, which is located at the cell surface. Epidermal growth factor (EGF), transforming growth factor (TGF-), amphiregulin, heparin-binding EGF, and betacellulin are just a few of the ligands that bind to and activate the EGFR.
The tyrosine kinase domain is activated by the receptors' formation of homo- or heterodimeric complexes after ligand binding. The Ras-Raf-MAP kinase, PI-3K/Akt, PKC, and Stat/Jak signaling pathways are all activated as a result of the dimerization and autophosphorylation of EGFR. The EGFR is activated to control cellular survival, differentiation, and proliferation. The EGFR has been derided as a proto-oncogene primarily because of its function in encouraging cell proliferation and preventing apoptosis.

EGFR related products

Structure Cat No. Product Name CAS No. Product Description
V69379 (3S,4S)-PF-06459988 1858291-14-1 (3S, 4S)-PF-06459988 is the less active S-enantiomer of PF-06459988.
V83079 (±)-Norcantharidin 29745-04-8 (±)-Norcantharidin (Endothall anhydride) is a synthetic anticancer agent that functions as a dual inhibitor of EGFR and c-Met in human colon cancers.
V69423 2′-Thioadenosine (PD157432) 136904-69-3 2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2 with IC50 of 45 µM for ErbB-2.
V77564 2-2(t)aptamer sodium 2-2(t) aptamer sodium is a trimeric complex of nucleic acid aptamer (2-2), containing 42 nucleotides, targeting ErbB-2.
V2347 4557W 179248-61-4 4557Wis a potent and reversible inhibitor of EGFR(Epidermal growth factor receptor) and c-ErbB2 (IC50s = 20 and 79 nM, respectively).
V3500 AC480 HCl 873837-23-1 AC480 HCl (also known as BMS-599626 HCl) is a novel, potent, orally bioavailable, selective and efficacious inhibitor of HER1 and HER2 (human epidermal growth factor receptors) with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.
V5152 AG-494 (Tyrphostin AG-494) 133550-35-3 AG-494 (formerly also known as Tyrphostin AG-494) is a novel and potent inhibitor of epidermal growth factor receptor (EGFR) kinase with an IC50 value of 1 µM in HT-22 cells
V5151 AG1478 HCl (Tyrphostin AG-1478) 170449-18-0 AG-1478 HCl (also known as Tyrphostin AG-1478) is a novel, potent and selective EGFR (epidermal growth factor receptor) inhibitor with IC50 of 3 nM in cell-free assays.
V34046 Allitinib tosylate 1050500-29-2 Allitinibtosylate (formerly AST-1306;AST1306; AST 1306), the tosylate ofAllitinib, is a selective and covalent/irreversible inhibitor of EGFR and ErbB2 with potential anticancer activity.
V31659 Almonertinib (HS-10296) hydrochloride 2134096-03-8 Almonertinib hydrochloride (HS10296)is a novel, potent, orally bioavailable, 3rd-generation irreversible inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity.
V69331 Amivantamab (JNJ-61186372) 2171511-58-1 Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune and anti-cancer activity.
V69441 Anbenitamab (KN-026) 2367012-88-0 Anbenitamab (KN-026) is a bispecific antibody that targets both extracellular domains II and IV of human HER2.
V69392 Antiproliferative agent-34 2910858-34-1 antiproliferation agent-34 (Compound A14) is a multi-target kinase inhibitor (antagonist) with IC50s of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT, respectively.
V2759 ARRY-380 analog 937265-83-3 ARRY-380 analog, an analog of ARRY-380 (Irbinitinib, formerly known as ARRY-380 andONT-380 or Tucatinib) which is a potent and selective small molecule inhibitor of HER2 with IC50 value of 8 nM, it is equally potent against truncated p95-HER2, and is 500-fold more selective for HER2 versus EGFR.
V11916 AV-412 Tosylate 451493-31-5 AV-412 Tosylate (also known as AV412; MP-412), the tosyulate salt of AV412, is a novel, 2nd generation and orally bioavailable EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
V3695 Avitinib (AC0010) maleate 1557268-88-8 Avitinib maleate (formerly also known as AC-0010, AC0010MA; Abivertinib), themaleate salt of avitinib, is an orally bioavailable and covalent/irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor selective for T790M resistance mutations.
V69369 AZ-5104-d2 2719691-01-5 AZ-5104-d2 is the deuterium labelled form of AZ-5104.
V4280 AZ7550 1421373-99-0 AZ7550 (AZ-7550; AZ 7550) is an active metabolite ofAZD-9291 (Osimertinib, a marketed anticancer drug)which inhibits the activity ofIGF1Rwith anIC50of 1.6 μM.
V4281 AZ7550 hydrochloride 2309762-40-9 AZ7550 HCl, the hydrochloride salt of AZ-7550, is N-demethylated(one of the methyl groups is removed from the ethyl diamine side chain) and active metabolite ofAZD9291 (Osimertinib), which is approved anticancer drug that inhibits IGF1Rwith anIC50of 1.6 μM.
V4282 AZ7550 Mesylate 2319837-99-3 AZ7550 Mesylate (AZ-7550), the mesylate salt ofAZ 7550, is an active metabolite ofAZD-9291 (Osimertinib) by removing one of the methyl groups from the ethyl diamine side chain.
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