|Description||Doxorubicin is an anthracycline antibiotic with antineoplastic activity. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the hydroxylated congener of daunorubicin. Doxorubicin intercalates between base pairs in the DNA helix, thereby preventing DNA replication and ultimately inhibiting protein synthesis. Additionally, doxorubicin inhibits topoisomerase II which results in an increased and stabilized cleavable enzyme-DNA linked complex during DNA replication and subsequently prevents the ligation of the nucleotide strand after double-strand breakage. Doxorubicin also forms oxygen free radicals resulting in cytotoxicity secondary to lipid peroxidation of cell membrane lipids; the formation of oxygen free radicals also contributes to the toxicity of the anthracycline antibiotics, namely the cardiac and cutaneous vascular effects.|
|Synonyms||JNS002; JNS-002; doxorubicin;|
|Current Developer||Janssen Pharmaceutical K.K.|
Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. It is a drug used in cancer chemotherap...
Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM. It is chemotherapeutic of the anthracycline family that is g...
Maytansinol disrupts the mitotic spindle and prevents mitotic exit in Drosophila used in the preparation of site-specific trastuzumab maytansinoid antibody-drug...
The cytotoxicity of PNU-159682 were in the subnanomolar range (0.07-0.58 nmol/L) and noticeably lower than that recorded for both MMDX and doxorubicin; PNU-1596...
Ansamitocin P-3, a metabolite of Ansamitocin, displays potent cytotoxicity against as a a new maytansinoid antitumor antibiotic.
Dolastatin 10 is an inhibitior of microtubule disassembly (IC50= 1.2μM) and potently inhibits vincristine binding to tubulin in a noncompetitive manner ( Ki= 1....
HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in ...
MMAD is a highly potent inhibitor of tubulin.
Methotrexate, a folate antagonist, is a potent anti-inflammatory agent when used weekly in low concentrations, the anti-phlogistic action of which is due to inc...
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility. It induced mitotic cell cycle ar...
MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monome...
MMAF is an antitubulin agent that inhibit cell division by blocking the polymerization of tubulin and it has lower cytotoxic activity than MMAE. It is an antibo...
Tubulysin A is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays. Tubulysin A is a novel antibiotic, which is anti-mi...
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human ...
alpha-Amanitin, the major toxic bicyclic octapeptide of the mushroom Amanita phalloides, inhibits RNA polymerase II at 1 µg/ml, RNA polymerase III at 10 µg/ml a...
Daunorubicin hydrochloride is the hydrochloride salt of an anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Dau...
Triptolide is a diterpenoid epoxide found in the Thunder God Vine, Tripterygium wilfordii, which has been used in traditional Chinese medicine for more than two...
Doxorubicin is an anthracycline antibiotic with antineoplastic activity. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the hy...
For comparison purposes, the ADC A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was conjugate...
MMAE, whose full name is Monomethyl auristatin E, inhibits tubulin polymerization so that it inhibits cell division.