|
|
Anti-Tumor Agents by Mechanisms of Action |
 |
Cancer Research |
|
 |
| |
|
| Angiogenesis Inhibitors |
| Name |
Biological activity |
Prod No. |
| Angiostatin K1-3 |
A proteolytic fragment of plasminogen that is a specific inhibitor of endothelial cell growth and angiogenesis. |
A1477 |
| DL-α-Difluoromethyl-ornithine |
Irreversible inhibitor of ornithine decarboxylase (ODC); chemoprotective agent that blocks angiogenesis. |
D193 |
| Endostatin |
Potent inhibitor of angiogenesis and tumor growth; inhibits endothelial cell proliferation. |
E8154
E8279
|
| Fumagillin |
Inhibitor of endothelial cell proliferation and angiogenesis. |
F6771 |
| Genistein |
Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis. |
G6649
G6776 |
| Minocycline |
Inhibits endothelial cell proliferation and angiogenesis. |
M9511 |
| Staurosporine |
Blocks angiogenesis by inhibiting the upregulation of VEGF expression in tumor cells. |
S4400 |
| (±)-Thalidomide |
Selectively inhibits biosynthesis of tumor necrosis factor α (TNF-α); inhibits angiogenesis. |
T144 |
| DNA Intercalators / Cross-linkers |
back to top |
| Name |
Biological activity |
Prod No. |
| Bleomycin |
Inhibits DNA synthesis and causes cleavage at specific base sequences. Induces apoptosis in a variety of cells; inhibits tumor angiogenesis. |
B5507
B2434 |
| Carboplatin |
Forms cytotoxic adducts with DNA; induces apoptosis. |
C2538 |
| Carmustine |
DNA alkylating/crosslinking agent effective against glioma and other solid tumors. |
C0400 |
| Chlorambucil |
Alkylates DNA; induces apoptosis of leukemia cells by a p53-dependent mechanism. |
C0253 |
| Cyclophosphamide |
Cytotoxic nitrogen mustard that crosslinks DNA and causes strand breakage. |
C0768
C7397 |
| cis-Diammineplatinum(II) dichloride (Cisplatin) |
Forms cytotoxic adducts with the DNA dinucleotide d(pGpG); induces apoptosis. |
P4394 |
| Melphalan |
Forms DNA intrastrand crosslinks by alkylation of 5'-(GGC) sequences. |
M2011 |
| Mitoxantrone |
DNA intercalating agent that inhibits DNA synthesis |
M6545 |
| Oxaliplatin |
Cytotoxicity follows the formation of adducts with DNA. |
O9512 |
| DNA Synthesis Inhibitors |
back to top |
| Name |
Biological activity |
Prod No. |
| (±)-Amethopterin (Methotrexate) |
Folic acid antagonist; blocks thymidine biosynthesis by inhibiting dihydrofolate reductase. |
A7019 |
| 3-Amino-1,2,4-benzotriazine 1,4-dioxide |
Hypoxia-activated antineoplastic agent. |
A9938 |
| Aminopterin |
Folic acid antagonist; blocks thymidine biosynthesis by inhibiting dihydrofolate reductase. More potent, but more toxic, than methotrexate. |
A1784 |
| Cytosine β-D-arabinofuranoside |
Selective inhibitor of DNA synthesis. |
C1768
C6645 |
| 5-Fluoro-5'-deoxyuridine |
Inhibits proliferation of tumors, cell lines or fibroblasts transformed by H-Ras or Trk oncogenes. |
F8791 |
| 5-Fluorouracil |
Inhibits thymidylate synthetase and depletes dTTP; it forms nucleotides that can be incorporated into RNA and DNA and induces p53-dependent apoptosis. |
F6627 |
| Ganciclovir |
In suicide gene therapy of solid tumors, the gene for Herpes simplex virus thymidine kinase is delivered to tumor cells and expressed, which in turn activates ganciclovir cytotoxicity. |
G2536 |
| Hydroxyurea |
Inactivates ribonucleoside reductase and blocks the synthesis of deoxynucleotides, thus inhibiting DNA synthesis and inducing cell death. |
H8627 |
| Mitomycin C |
Inhibits DNA synthesis, nuclear division, and proliferation of cancer cells. |
M0503 |
| DNA-RNA Transcription Regulators |
back to top |
| Name |
Biological activity |
Prod No. |
| Actinomycin D |
Inhibits cell proliferation by complexing to DNA and blocking the production of mRNA by RNA polymerase; induces apoptosis. |
A1410 |
| Daunorubicin |
Complexes to DNA and blocks production of mRNA by RNA polymerase. |
D8809 |
| Doxorubicin |
Binds to DNA and inhibits reverse transcriptase and RNA polymerase. |
D1515 |
| Homoharringtonine |
Binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. |
H0635 |
| Idarubicin |
Anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin. |
I1656 |
| Enzyme Inhibitors |
back to top |
| Name |
Biological activity |
Prod No. |
| S(+)-Camptothecin |
Binds irreversibly to the DNA-topoisomerase I complex leading to the irreversible cleavage of DNA and the destruction of cellular topoisomerase I by the ubiquitin-proteasome pathway. Induces apoptosis in many normal and tumor cell lines.
|
C9911 |
| Curcumin |
Potent inhibitor of protein kinase C, EGFR tyrosine kinase and IκB kinase. Induces apoptosis in cancer cells. |
C7727 |
| (-)-Deguelin |
Inhibitor of activated Akt. Does not affect MAPK, ERK1/2 or JNK. |
D0817 |
| 5,6-Dichlorobenz-imidazole 1-β-D-ribofuranoside |
Inhibitor of RNA synthesis, causes premature termination of transcription. |
D1916 |
| Etoposide |
Binds to the DNA-topoisomerase II complex to enhance cleavage and inhibit religation; inhibits synthesis of the oncoprotein Mdm2 and induces apoptosis in tumor lines that overexpress Mdm2. |
E1383 |
| Formestane |
Aromatase inhibitor |
F2552 |
| Fostriecin |
Interferes with the reversible phosphorylation of proteins that are critical for progression through the cell cycle. |
F4425 |
| Hispidin |
Potent inhibitor of protein kinase Cβ. |
H5257 |
| 2-Imino-1-imidazoli-dineacetic acid (Cyclocreatine) |
Creatine analog; decreases the rate of ATP production via creatine kinase and reduces the proliferation of tumor cell lines characterized by high levels of creatine kinase expression. |
37,762-7 |
| Mevinolin |
Inhibits mevalonic acid production and induces apoptosis in numerous cancer cell lines, perhaps, in part, by inhibiting the isoprenylation of Rho-family GTPases. |
M2147 |
| Trichostatin A |
Histone deacetylase inhibitor that enhances the cytotoxic efficacy of anticancer drugs that target DNA. |
T8552 |
| Tyrphostin AG 34 |
Tyrosine protein kinase inhibitor in human colon cancer cell lines. |
T6318 |
| Tyrphostin AG 879 |
Inhibits the tyrosine kinase activity of the nerve growth factor receptor (TrkA; pp140trk) and heregulin receptor erbB-2. |
T2067 |
| Gene Regulation |
back to top |
| Name |
Biological activity |
Prod No. |
| 5-Aza-2'-deoxycytidine |
Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes. |
A3656 |
| 5-Azacytidine |
A2385 |
| Cholecalciferol (Vitamin D3) |
Antiproliferative action on breast, prostate, and colon cancer cells |
C9756 |
| 4-Hydroxytamoxifen |
Metabolite of tamoxifen that is a potent selective estrogen response modifier (SERM); the trans (Z) isomer has efficacy against estrogen-sensitive cancers. The cis (E) isomer is an estrogen agonist. |
H6278 |
| Melatonin |
Enhances apoptotic death of cancer cells; inhibits proliferation/metastasis of breast cancer cells by inhibiting estrogen receptor action. |
M5250 |
| Mifepristone |
Progesterone receptor antagonist; stimulates prolactin secretion. Pgp inhibitor. |
M8046 |
| Raloxifene |
Selective estrogen response modifier (SERM), may have efficacy against estrogen-sensitive cancers. |
R1402 |
| all trans-Retinal (Vitamin A aldehyde) |
Ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells. |
R2500 |
| Retinoic acid, all trans (Vitamin A acid) |
R2625 |
| 9-cis-Retinoic Acid |
R4643 |
| 13-cis-Retinoic acid |
R3255 |
| Retinol (Vitamin A) |
R7632 |
| Tamoxifen |
Selective estrogen response modifier (SERM), used therapeutically and prophylactically against estrogen-sensitive tumors. |
T5648
T9262 |
| Troglitazone |
Anti-tumor agent; PPAR-γ agonist; induces apoptosis via a p53 pathway. |
T2573 |
| Microtubule Inhibitors |
back to top |
| Name |
Biological activity |
Prod No. |
| Colchicine |
Antimitotic agent that disrupts microtubules by binding to tubulin and preventing its polymerization; induces apoptosis in several normal and tumor cell lines. |
C9754 |
| Dolastatin 15 |
Reported to interact with tubulin and induce apoptosis.
|
D5566 |
| Nocodazole |
Antimitotic agent that binds to β-tubulin and disrupts mitotic spindle function; induces apoptosis in several normal and tumor cell lines. |
M1404 |
| Paclitaxel |
Binds to β-tubulin and promotes the formation of highly stable microtubules that resist depolymerization, preventing cell division. |
T7191
T7402
T1912 |
| Podophyllotoxin |
Inhibits microtubule assembly. |
P4405 |
| Rhizoxin |
Binds to β-tubulin in most eucaryotic cells including animals, plants and fungi. It completely prevents formation of an intrachain cross-link in β-tubulin by N,N'-ethylenebis(iodoacetamide). |
R8149 |
| Vinblastine |
Antimitotic agent. Inhibits microtubule assembly by binding tubulin and inducing self-association; depolymerizes pre-existing microtubules. Induces apoptosis in several tumor cell lines. |
V1377 |
| Vincristine |
V8879 |
| Vindesine |
V8254 |
| Vinorelbine (Navelbine) |
Potent anti-mitotic, anti-tumor agent. Low neurotoxicity is related to its higher affinity for mitotic microtubules than for axonal microtubules. |
V2264 |
| Other Antitumor Agents |
back to top |
| Name |
Biological activity |
Prod No. |
| 17-(Allylamino)-17-demethoxygeldanamycin |
Inhibits the activity of oncogenic proteins such as N-ras, Ki-ras, c-Akt, and p185erB2. Induces apoptosis. |
A8476 |
| 4-Amino-1,8-naphthalimide |
Sensitizes cells to radiation-induced cell damage and enhances the cytotoxicity of 1-methyl-3-nitro-1-nitrosoguanidine. |
A0966 |
| Apigenin |
Inhibits cell proliferation by arresting the cell cycle at the G2/M phase. Inhibition of growth through cell cycle arrest and induction of apoptosis appear to be related to induction of p53. Inhibitory effects on tumor promotion may also be due to inhibition of kinase activity and the resulting suppression of oncogene expression. It has also been reported to inhibit topoisomerase I catalyzed DNA religation and enhance gap junctional intercellular communication. |
A3145 |
| Brefeldin A |
Disrupts the structure and function of the Golgi apparatus. An activator of the sphingomyelin cycle. |
B7651 |
| Cimetidine |
H2 histamine receptor antagonist; I1 imidazoline receptor agonist; anti-ulcer agent. Blocks cancer metastasis by inhibiting the expression of E-selectin on the surface of endothelial cells, thus blocking tumor cell adhesion. |
C4522 |
| Dichloromethylene-diphosphonic acid |
Analog of pyrophosphate ion that inhibits the osteoclastic activity leading to bone resorption and osteoporosis. Found also to inhibit collagenase and matrix metalloproteinase 1. |
D4434 |
| Leuprolide (Leuprorelin) |
Luteinizing hormone releasing hormone (LH-RH) agonist. |
L0399 |
| Luteinizing Hormone-Releasing Hormone |
Hypothalamic peptide that stimulates release of gonadotrophins from anterior pituitary, thus regulating reproductive functions. |
L7134 |
| Pifithrin-α |
Reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1 and mdm2 expression. Enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. |
P4359 |
| Rapamycin |
Inhibition of the molecular target of rapamycin (mTOR) mediates the antiproliferative and anticancer activity of rapamycin by blocking the PI3K/Akt pathway. |
R0395 |
| Sex hormone-binding globulin |
Regulates the availability of sex steroid hormones and limits their access to target cells. Inhibits estradiol-induced proliferation of breast cancer cells. |
S1437 |
| Thapsigargin |
Cytotoxin that induces apoptosis by disrupting intracellular free Ca2+ levels. |
T9033 |
| Urinary trypsin inhibitor fragment (Bikunin) |
Blocks the metastasis of human ovarian cell line (HRA) without affecting their proliferation. |
U4751 |
Back to Cancer Research Home
|
|
|
