escc

Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Ethyl 3,4-dihydroxybenzoate (EDHB): a prolyl hydroxylase inhibitor attenuates acute hypobaric hypoxia mediated vascular leakage in brain.

PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

ZSH-2208, an analogue of retinoic acid A, exerts strong anti-tumor effects on regenerative stem cells (TRCs) in esophageal squamous cell carcinoma (ESCC) via the RARγ-TNFAIP3 pathway.

Camrelizumab (SHR-1210) is a human IgG4-κ monoclonal antibody with high affinity directed against PD-1, binding PD-1 with an affinity of up to 3 nM and inhibiting PD-1 PD-L1 with an IC50 of 0.70 nM. Camrelizumab exhibits anti-tumor activity and is well tolerated in cancers, including NSC-LC, ESCC, Hodgkin's lymphoma, and advanced HCC.

TAPI1 acetate is a salt form of TAPI1. TAPI1 (TNF-α processing inhibitor-1) is a TACE (ADAM17) inhibitor that inhibits shedding of TNF-α, TNFRI (p60), and TNFRII (p80), IL-6 other cytokine receptors; TAPI-1 is also a metalloproteinase MMP inhibitor that promotes cisplatin-induced ESCC cell apoptosis by inhibiting the NF-κB signaling pathway to promote cisplatin-induced apoptosis in ESCC cells.

Afatinib (BIBW 2992) oxalate is an irreversible, orally active bispecific inhibitor of the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFRwt, 0.4 nM for EGFRL858R, 10 nM for EGFRL858R T790M, and 14 nM for HER2. Afatinib oxalate can be used to study esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer.

(R)-Afatinib ((R)-BIBW 2992), an isomer of Afatinib, is a potent, orally administered, irreversible inhibitor targeting the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFR wt, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R T790M, and 14 nM for HER2, holding potential for research into esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer [1].

ERK-IN-6 (compound 6g) is a potent anti-proliferative agent against esophageal squamous cell carcinoma (ESCC), inducing apoptosis via the ERK pathway, with potential applications in ESCC research [1].

Xerophilusin B, isolated from Isodon xerophilus as an anticancer agent, demonstrates antiproliferative effects on esophageal squamous cell carcinoma (ESCC) cell lines. It induces G2 M cell cycle arrest and mediates apoptosis [1].

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

Picrasidine Q has the capacity of anti-cell transformation and anti-cancer, it might be a chemopreventive and chemotherapeutic agent by direct targeting FGFR2 and inhibiting cell proliferation of ESCC cells.