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.
Structure | Cat No. | Product Name | CAS No. | Product Description |
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V69379 | (3S,4S)-PF-06459988 | 1858291-14-1 | (3S, 4S)-PF-06459988 is the less active S-enantiomer of PF-06459988. |
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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. |
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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. |
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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. | |
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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). |
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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. |
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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 |
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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. |
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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. |
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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. |
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V69369 | AZ-5104-d2 | 2719691-01-5 | AZ-5104-d2 is the deuterium labelled form of AZ-5104. |
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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. |
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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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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. |
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V12121 | AZD9291DA | 1421372-66-8 | AZD9291-DA (also known asMutated EGFR-IN-1 or Osimertinib analog)is a des acryl analogue of AZD9291, which is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. |
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V69333 | BAY 2476568 | 2311901-93-4 | BAY 2476568 is a highly efficient and selective EGFR inhibitor (antagonist) with IC50 of < 0.2 nM against wild-type EGFR and mutant EGFR. |
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V69378 | BEBT-109 | 2050906-40-4 | BEBT-109 is a potent pan-mutation-selective EGFR inhibitor. |
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V69398 | Becotatug (JMT-101) | 2648260-93-7 | Becotatug (JMT-101) is an IgG1 antibody targeting EGFR and can also be coupled with Afatinib and Osimertinib to form an ADC. |
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V69334 | Befotertinib (D-0316) | 1835667-63-4 | Befotertinib (D-0316) is a third-generation EGFR tyrosine kinase inhibitor. |
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V2934 | BIBX 1382 | 196612-93-8 | Falnidamol (formerly known as BIBX 1382) is a potent and selective inhibitor EGFR inhibitor with IC50 of 3 nM and potential anticancer activities; it displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). |