antitumor activity

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

PCI-24781 (Abexinostat (PCI24781)) is a new pan-HDAC inhibitor mainly targeting HDAC1 (Ki: 7 nM), also have moderate inhibitory for HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.

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.

(R)-Naproxen, an anti-inflammatory agent, has antipyretic and analgesic properties. Both the acid and its sodium salt are used in the therapy of acute gout or dysmenorrhea, musculoskeletal disorders, rheumatoid arthritis and other rheumatic.

Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting.

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a highly selective, potent competitive inhibitor of P-glycoprotein (P-gp, ABCB1) with a Ki value of 59 nM. Zosuquidar trihydrochloride exhibits antitumor activity and can be used in research on tumors such as leukemia.

DM1-SMe (DM1-SSMe) is a potent inhibitor of maytansinoid microtubular. DM1-SMe is about 3 to 10-fold more potent than the parent drug Maytansine, with IC50s of 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines.

1. Peimisine (Ebeiensine) can affect M-receptor, excit β-receptor, restrain the release of internal calcium, and promote to releaseing nitrogen monoxidum in order to relax tracheal smooth muscle and relieve asthma. 2. Peimisine can attenuate lung tissue injury( ALI), LDH and MDA amount in ALI mice in a dose dependent manner, it also lower the total protein, total white blood cells, lymphocyte and neutrophilic leukocyte in bronchoalveolar lavage fluid( BALF); suggests that peimisine can play a protective role against LPS-induced acute lung injury. 3. Peimisine has the protective effect on the experimental hepatic fibrosis formation, the possible mechanisms are associated with inhibiting fibrogenesis and fibrosis accumulation, and decreasing lipid peroxidation. 4. Peimisine can inhibit angiotensin I converting enzyme activity in a dose-dependent manner, displaying 5 % inhibitory concentration values of 526.5 microM, thus, it may have antihypertensive action.

Magrolimab (Hu5F9-G4) is a humanized anti-CD47 IgG4 monoclonal antibody that exhibits antitumor activity by blocking CD47 and binding primarily to the N-terminal pyroglutamate of CD47. It can be used in combination with other compounds for the treatment of recurrent myeloma.

Sacituzumab (hRS7) is an antibody inhibitor and a humanized monoclonal antibody targeting trophoblast cell surface antigen 2 (TROP2), serving as a component of the antibody-drug conjugate sacituzumab govitecan, used for research and treatment of TROP2-high-expressing tumors such as triple-negative breast cancer.

Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate functioning as a HER2-targeted topoisomerase I inhibitor, with targeting capability and antitumor activity, employed in research on HER2-positive breast cancer and gastric cancer.

Datopotamab deruxtecan (DS-1062) is an antibody-drug conjugate (ADC) that targets tropomyosin 2 (TROP2) on the surface of trophoblast cells. Datopotamab deruxtecan exhibits antitumor activity by specifically binding to TROP2 and internalizing, releasing DXd to inhibit topoisomerase I (IC₅₀ = 0.31 μM), thereby inducing DNA damage and apoptosis. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

Zolbetuximab(IMAB362) is a monoclonal antibody that specifically targets Claudin-18.2.Zolbetuximab has potential antitumor activity, mediating killing of Claudin-18.2-positive cells through an immune effector mechanism.Zolbetuximab is used in the study of gastrointestinal adenocarcinomas and pancreatic tumors.

Atezolizumab is an antibody inhibitor, a humanized monoclonal antibody, IgG1, which targets PD-L1 and blocks the interaction of PD-L1 with PD-1. Atezolizumab has antitumor activity and promotes T-cells to attack tumor cells.

Avelumab is a humanized anti-PD-L1 monoclonal antibody that binds to PD-L1 with high specificity (Kd = 0.1 nM) and exhibits potential antibody-dependent cell-mediated cytotoxicity (ADCC). Avelumab exerts a dual mechanism of action, combining direct antitumor activity with ADCC. Avelumab is used in research on cancers such as Merkel cell carcinoma.

Bevacizumab, a humanized monoclonal antibody, specifically and with high affinity binds to all isoforms of VEGF-A.

Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.

Ipilimumab (Yervoy) is an antibody inhibitor that blocks the inhibitory receptor cytotoxic T-lymphocyte antigen-4 (CTLA-4) on T cells, with immune-activating properties. Used for the treatment of unresectable or metastatic melanoma, this antibody exhibits antitumor activity.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.