Hsdb 7454
CAS: 205923-56-4
Molecular Formula: C107H179N35O36S7
Hsdb 7454 - Names and Identifiers
Hsdb 7454 - Physico-chemical Properties
| Molecular Formula | C107H179N35O36S7 |
| Molar Mass | 2756.23406 |
| Storage Condition | 4°C,Do not freeze |
| In vitro study | Cetuximab (anti-EGFR) is a recombinant chimeric monoclonal antibody with high affinity for the human EGFR receptor. It binds to EGFR and inhibits the phosphoactivation of its receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, and reduced production of VEGF. Cetuximab has a significant single-agent anti-tumor effect, with an additive effect with cisplatin or paclitaxel in NPC cell lines with high expression of EGFR protein, but not on NPC cell lines with low expression of EGFR (such as CNE-2 and C666-1). Has little effect. Cetuximab prevents EGFR from interacting with the ligand, inhibiting downstream RAS-ERK activation. It can promote the endoplasmic reticulum stress response (ER stress), promote ER protein transport to the cell membrane. It competitively inhibits ligand binding and inhibits tyrosine kinase activation, resulting in receptor down-regulation. In addition to competitive inhibition, binding of cetuximab to EGFR may cause internalization and destruction of the receptor. |
| In vivo study | In mouse xenograft models, Cetuximab was able to enhance the antitumor activity of several chemotherapeutic drugs. It exerts its anti-tumor effects through a variety of mechanisms, including inhibiting cell cycle progression, arresting the cell cycle in G1 phase, and reducing the number of cells in S phase. The arrest of cells in the G1 phase by Cetuximab can also cause apoptosis by inducing and activating related pro-apoptotic molecules. Administration alone or in combination with carboplatin resulted in decreased tumor size, decreased metastatic spread, decreased cell surface expression of EGFR, MVD in NCI-N87 tumors without BRAF and K-ras mutations. It has little effect in tumors derived from MKN-45 (the tumor phenotype is predominant in BRAF and K-ras, but weakly expressed in cytoplasmic EGFR). |
Hsdb 7454 - Introduction
Cetuximab is a monoclonal antibody, which can inhibit EGFR. SPR method shows that the Kd value of Cetuximab to soluble EGFR is 0.201 nM. Cetuximab has high anti-tumor effect.
Last Update：2022-10-16 17:40:21
