The epidermal growth factor receptor (EGFR; ErbB1) is a member of the epidermal growth factor RTK (receptor tyrosine kinases) family, which also includes HER2/neu (ErbB2), ErbB3 (HER3), and ErbB4 (HER4). 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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V2695 | Nazartinib (EGF816, NVS-816) | 1508250-71-2 | Nazartinib (formerly known as EGF816, NVS-816) is a novel, covalent/irreversible, mutant-selective EGFR inhibitor with Kiand Kinactof 31 nM and 0.222 min−1on EGFR(L858R/790M) mutant, respectively. |
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V0537 | Neratinib (HKI-272; PB272; Nerlynx) | 698387-09-6 | Neratinib (formerly known as HKI-272 or PB-272; trade name:Nerlynx)is a highly potent, selective, and orally bioavailable HER2 and EGFR inhibitor with potential antitumor activity. |
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V3916 | NERATINIB MALEATE | 915942-22-2 | Neratinib maleate, the maleate salt of neratinib (HKI-272; PB-272;Nerlynx), is an orally bioavailable HER2 and EGFR inhibitor approved by FDA in 2017 to reduce the risk of breast cancer returning. |
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V0562 | OSI-420 (Desmethyl Erlotinib) HCl | 183320-51-6 | OSI-420 HCl (also known as CP-473420; OSI420; Desmethyl Erlotinib), the demethylated and active metabolite of erlotinib, is a potent, selective, orally bioavailable and ATP competitive inhibitor of tyrosine kinase EGFR with potential antineoplastic activity. |
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V0546 | Osimertinib (AZD9291; Tagrisso) | 1421373-65-0 | Osimertinib (formerly AZD-9291 and mereletinib; trade name Tagrisso) is an oral bioavailable, irreversible/covalent, and mutant-selective EGFR inhibitor with potential antineoplastic activity. |
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V3976 | OSIMERTINIB DIMESYLATE | 2070014-82-1 | Osimertinib dimesylate (mereletinib;AZD 9291;AZD9291; AZD-9291; trade name Tagrisso), the dimesylate salt of osimertinib, is an oral bioavailable and covalent/irreversible EGFR inhibitor approved as a cancer treatment in 2017 by both the Food and Drug Administration and the European Commission. |
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V3975 | OSIMERTINIB MESYLATE | 1421373-66-1 | Osimertinib mesylate (formerly known as AZD9291; AZD-9291; AZD 9291; mereletinib; Tagrisso), the mesylate salt of osimertinib, is a novel, potent, oral bioavailable, irreversible, and mutant-selective, 3rd generation EGFR inhibitor approved by both FDA and the European Commission for cancer treatment. |
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V0568 | PD153035 HCl (SU5271; ZM252868) | 183322-45-4 | PD153035 HCl (SU-5271; ZM-252868), the hydrochloride salt of PD153035(also called PD-153035), is an ATP competitive EGFR inhibitor with potential antineoplastic activity. |
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V0547 | PD168393 (PD-168393) | 194423-15-9 | PD168393 (PD-168393)is covalent / irreversible, cell-permeable and ATP-competitive EGFR inhibitor with potential anticancer activity. |
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V0553 | Pelitinib (EKB-569; WAY-EKB 569) | 257933-82-7 | Pelitinib (formerly EKB569; WAY-EKB569; WAY-172569), a 3-cyanoquinoline analog, is an irreversible/covalent EGFR inhibitor with potential antineoplastic activity. |
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V0545 | Poziotinib (HM781-36B) | 1092364-38-9 | Poziotinib (formerly known as HM781-36B, NOV120101, HM781 36B) is a novel, potent, orally bioavailable, quinazoline-based, irreversible/co-valent pan-inhibitor of HER (human epidermal growth factor receptor 2) with potential antitumor activity. |
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V9597 | RG 13022 | 136831-48-6 | RG13022 is a tyrosine kinase inhibitor (TKI); the IC50 for inhibiting EGF receptor autophosphorylation is 4 μM. |
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V0551 | Rociletinib (CO-1686, AVL-301, CNX-419) | 1374640-70-6 | Rociletinib (formerly CO1686; AVL301; CNX419) is an orally bioavailable, covalent / irreversible, and mutant-selective EGFR (e.g. T790M) inhibitor with potential antineoplastic activity. |
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V0567 | Sapitinib (AZD-8931) | 848942-61-0 | Sapitinib (formerly AZD8931; AZD-8931) is an orally bioactive, reversible and ATP competitive inhibitor of multiple kinases including EGFR, ErbB2/3 with potential antitumor activity. |
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V0555 | TAK-285 | 871026-44-7 | TAK-285 (TAK285), currently being investigated by Takeda company, is a dual HER2/EGFR(HER1) inhibitor with potential antitumor activity. |
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V15759 | Tarloxotinib bromide | 1636180-98-7 | Tarloxotinib bromide (formerly TH-4000; PR-610) is a novel quarternary amine-based and irreversible EGFR/HER2 inhibitor designed as a prodrug to selectively release a covalent (irreversible (covalent)) EGFR tyrosine kinase inhibitor under severe hypoxia, a feature of many solid tumors. |
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V4153 | Theliatinib (HMPL309) | 1353644-70-8 | Theliatinib (formerly HMPL-309; HMPL309;HMPL 309;xiliertinibum; xiliertinib) is a novel and highly potent EGFR-TKI (epidermal growth factor receptor-tyrosine kinase inhibitor) withpotential antitumor and anti-angiogenesis activities. |
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V0564 | Tyrphostin 9 (AG17; Malonoben) | 10537-47-0 | Tyrphostin-9 (also named as Malonoben; SF-6847; RG-50872; AG-17; GCP-5126; NSC-242557) is a novel and potent epidermal growth factor receptor (EGFR) inhibitor with potential anticancer activity. |
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V16970 | Tyrphostin AG-528 | 133550-49-9 | Tyrphostin AG-528 (Tyrphostin B66) is a PTK (protein tyrosine kinase) inhibitor (antagonist) with IC50 of 4.9 μM for epidermal growth factor receptor (EGFR) and IC50 of 2.1 μM for ErbB2. |
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V0570 | Varlitinib (ARRY-543; ARRY-334543; ASLAN-001) | 845272-21-1 | Varlitinib (formerly also known as ARRY543; ARRY-334543; ASLAN001) is a novel, potent, orally bioavailable, selective and reversible ErbB1 (EGFR) and ErbB2 (HER2) inhibitor with potential antitumor activity. |
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