Antineoplastic

Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with an IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. Imatinib is an oral chemotherapy agent used to treat cancers. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome-positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis, and myelodysplastic syndrome.

Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling. Regorafenib is demonstrated to increase the overall survival of patients with metastatic colorectal cancer and has been approved by the US FDA on September 27, 2012.

Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

4'-epi-Daunorubicin Hydrochloride is an impurity of Daunorubicin, which is an anthracycline antibiotic used in the treatment of acute myeloid and lymphocytic leukemia, with adverse reactions such as cardiotoxicity and bone marrow suppression.

Epirubicin EP Impurity F is an impurity of Epirubicin, which is an anthracycline topoisomerase inhibitor used as an antineoplastic agent.

Bortezomib is a potent, reversible and selective 20S proteasome inhibitor with a Ki of 0.6 nM. It is an antineoplastic agent that is used in treatment of refractory multiple myeloma and certain lymphomas.

Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. It is used for the treatment of colon and rectum cancers. It binds to topoisomerase I-DNA complex, preventing religation of the DNA strand and leading to double-strand DNA breakage and cell death.

Epirubicin, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. It is clinically active against a broad range of tumor types, including breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma and so on.

Bleomycin is complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2. It forms complexes with iron that reduce molecular oxygen to superoxide and hydroxyl radicals which cause single- and double-stranded breaks in DNA. It inhibits DNA metabolism and is used as an antineoplastic, especially for solid tumors. It is a medication used to treat cancer, including Hodgkin's lymphoma, non-Hodgkin's lymphoma, testicular cancer, ovarian cancer, and cervical cancer among others. It was initially developed by Bristol-Myers Squibb and has been listed.

Berubicin hydrochloride is the hydrochloride of berubicin, which is an anthracycline derivative used as a topoisomerase II inhibitor with activity in ependymoma. Berubicin hydrochloride has potential antineoplastic activity.

Distamycin is an anticancer antibiotic with antiviral and antiprotozoal activity.

Neocarzinostatin (NCS) is a macromolecular chromoprotein enediyne antitumor antibiotic produced by Str. carzinostatiuns var. neocarzinostaticus F41. It can resist gram-positive bacteria and is clinically used in acute myelogenous leukemia, acute lymphocytic leukemia, pancreatic cancer, etc.

Vinblastine, an inhibitor of nAChR, is a natural alkaloid isolated from the plant Vinca rosea Linn. It binds to tubulin and inhibits microtubule formation, leading to disruption of mitotic spindle assembly and arrest of tumor cells in the M-phase of the cell cycle. It may also interfere with the metabolism of amino acids, cyclic AMP, and glutathione. It is used to treat malignant lymphoma.

Isoliquiritigenin, a flavonoid from the root of Glycyrrhiza glabrat, inhibits aldose reductase with an IC50 of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC50 of 24.7 μm. It has antioxidant, anti-inflammatory, and anti-tumor activities.

Cryptophycin 1, produced by Nostoc sp. GSV 224, is a potent cytotoxic anti-microtubule agent. Cryptophycin 1 can induce cell apoptosis, and has anti-tumor activity and excellent anti-proliferation ability.

Telomostatin, originally isolated from the bacteria Streptomyces anulatus, is a potent and specific telomerase inhibitor that acts only on human telomere sequences and does not affect DNA polymerases or reverse transcriptases. Telomostatin induces the formation of basket-type G-quadruplex (G4) structures from hybrid-type G-quadruplexes in the telomeric region.

Ibrutinib is a potent and selective BTK inhibitor (IC50=0.5 nM).

O-Acetylbenzeneamidinocarboxylic acid is isolated from Gibberella saubinetii with antitumor activity. It has weak inhibitory effect on tumor cells.

Aclacinomycin is an anthracycline drug that is used in the treatment of cancer.

Actidione, an inhibitor of eukaryotic protein synthesis, is an antibiotic isolated from the beers of Streptomycin-producing strains of Streptomyces griseus. Actidione is used as a fungicide and anticancer drug.