Antineoplastic

PNU-159682 is a major active metabolite of nemorubicin (MMDX) in human liver microsomes. It is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity, and shows >3,000-fold cytotoxic than its parent compound (MMDX and doxorubicin). It is a more potent and well tolerated ADC cytotoxin than doxorubicin.

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.

Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest.

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.

Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Marizomib irreversibly binds to and inhibits the 20S catalytic core subunit of the proteasome by covalently modifying its active site threonine residues.

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.

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.

Paclitaxel is a compound with anti-tumor activity extracted from the Pacific yew tree Taxus brevifolia. Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

Capecitabine inhibits tumor growth and metastatic recurrence after resection of human hepatocellular carcinoma (HCC) in highly metastatic nude mice model. It is a chemotherapy medication used to treat breast cancer, gastric cancer and colorectal cancer.

Midostaurin is a multi-target protein kinase inhibitor being investigated for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). It is a semi-synthetic derivative of staurosporine, an alkaloid from the bacterium Streptomyces staurosporeus.

Streptozotocin is a monosaccharide antibiotic produced by Str. achromogenes 128 (NRRL 2697). It has antibacterial effect, and human serum and urine do not affect its activity. It can protect mice infected with Staphylococcus aureus, Pasteurella pestis and Proteus vulgaris. The same amount of antibiotic U-15774 can inhibit mouse sarcoma-180, sarcoma L5178Y, Walker-256 and Ehrlich carcinoma. Streptozotocin is a glucosamine-nitrosourea derivative, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. It is commonly used for the treatment of metastatic pancreatic islet cell carcinoma.

Irofulven is a semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle.

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 = 20 nM), DiFi humancolon cancer cells and MDA MB-468 human breast cancer cells.

Geldanamycin is a benzoquinone ansamycin antibiotic that inhibits heat shock protein 90 (HSP90). Geldanamycin has been shown to promote survival of neural stem cells from oxidative stress via inhibition of HSP90. It displays potent antineoplastic properties and inhibits myeloma cell growth.

Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM. Genistein is developed to be an antitumor agent. Genistein has antioxidant effect, it can be used in cosmetics material. It is a plant polyphenol that can inhibit tyrosinase, block melanin synthesis, reduce skin pigment intensity, absorb UV, prevent photoaging, reduce sun damage and age spot formation, and whiten and lighten spots. It also has the anti-glycation and antibacterial effect, can effectively improve skin tone and skin texture, prevent the generation of age spots, remove red bloodlines, and improve skin blood microcirculation.