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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
(3S,4S)-PF-06459988 V69379 (3S,4S)-PF-06459988 1858291-14-1 (3S, 4S)-PF-06459988 is the less active S-enantiomer of PF-06459988.
(±)-Norcantharidin 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.
2′-Thioadenosine (PD157432) 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.
2-2(t)aptamer sodium 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.
4557W 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).
AC480 HCl 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.
AG-494 (Tyrphostin AG-494) 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
Antiproliferative agent-34 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.
ARRY-380 analog 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.
AV-412 Tosylate 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.
AZ-5104-d2 V69369 AZ-5104-d2 2719691-01-5 AZ-5104-d2 is the deuterium labelled form of AZ-5104.
AZ7550 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.
AZ7550甲磺酸盐 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.
AZ7550盐酸盐 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.
AZD9291DA 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.
BAY 2476568 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.
BEBT-109 V69378 BEBT-109 2050906-40-4 BEBT-109 is a potent pan-mutation-selective EGFR inhibitor.
Becotatug (JMT-101) 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.
Befotertinib (D-0316) V69334 Befotertinib (D-0316) 1835667-63-4 Befotertinib (D-0316) is a third-generation EGFR tyrosine kinase inhibitor.
BIBX 1382 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).
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