|Description||ELR510444 is a potent microtube disruptor with potential anticancer activity. ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 potently inhibited cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibited the rate and extent of purified tubulin assembly, and displaced colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site. ELR510444 is not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines, suggesting that it circumvents both clinically relevant mechanisms of drug resistance to this class of agents. ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window.|
D-64131, under the IUPAC name (5-methoxy-1H-indol-2-yl)-phenylmethanone, is a 2-aroylindole derivatives that inhibits tubulin polymerization. In vitro: Inhibits...
Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
XRP44X, under the IUPAC name [4-(3-chlorophenyl)piperazin-1-yl]-(5-methyl-2-phenylpyrazol-3-yl)methanone, as an inhibitor of Tubulin it indirectly inhibits Net ...
ELR510444 is a potent microtube disruptor with potential anticancer activity. ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular m...
Vinblastine is inhibitor of nAChR and can inhibit the formation of microtubule. It is a natural alkaloid isolated from the plant Vinca rosea Linn. It binds to t...
Ixabepilone (also known as azaepothilone B, or BMS-247550) is an orally bioavailable microtubule inhibitor. Ixabepilone was a semisynthetic analogue of epothil...
EHT-6706 can target the colchicine-binding site to inhibit tubulin polymerization as a tubulin polymerisation inhibitor. It is under the development of Diaxonhi...
ABT 751, also called E7010, is a a novel bioavailable tubulin-binding and antimitotic agent (in neuroblastoma: IC50= 0.6–2.6 μM; in non-neuroblastoma cell line...
Dolastatin 10 is an inhibitior of microtubule disassembly (IC50= 1.2μM) and potently inhibits vincristine binding to tubulin in a noncompetitive manner ( Ki= 1....
CHM 1 is an apoptosis inducer with potent antitumor activity in human hepatocellular carcinoma. It inhibits tubulin polymerization in vitro and in vivo, and res...
Cevipabulin, is a small synthetic molecule of triazolopyrimidine derivative with potential antitumor activity. With a novel mechanism of action distinct from th...
ACI-35 is a liposome-based vaccine designed to stimulate a patient’s immune system to produce antibodies against the misfolded and phosphorylated pathogenic for...
Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 value of 9.8~18 nM in tumor cells under the development of Nereus Pharm...
Indibulin, also called D 24851, estabilizes tubulin polymerization (IC50 = 0.3 μM) and induces tumor cell cycle arrest and apoptosis. In vitro: blocking cell cy...
Fosbretabulin disodium is the disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combret...
Maytansine is a cytotoxic agent, originally isolated from the Ethiopian shrub Maytenus serrata. It inhibits the assembly of microtubules by binding to tubulin a...
Epothilone D is a natural polyketide compound isolated from the myxobacterium Sorangium cellulosum. Also known as desoxyepothilone B, epothilone D binds to tubu...
Triclabendazole is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.
INDY，under the IUPAC name 1-(3-ethyl-5-hydroxy-1,3-benzothiazol-2-ylidene)propan-2-one, is a DYRK1A/B inhibitor (DYRK1B: IC50= 0.23μM; DYRKA: IC50= 0.230.24μM)....
Vinflunine, a semisynthetic derivative of Vinorelbine, is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family endowed with uniqu...