Epothilone b (Patupilone)
Anti cancer drug
10 vials of 10mg
For prostate cancer and other aggressive cancer forms.
This is for research purposes only.
Use 1 vial for 5 consecutive days followed by 21 days off before repeating.
The principal mechanism of the epothilone class is inhibition of microtubule function. Microtubules are essential to cell division, and epothilones therefore stop cells from properly dividing.
Epothilone B (patupilone) possess the same biological effects as paclitaxel both in vitro and in cultured cells. This is because they share the same binding site, as well as binding affinity to the microtubule. Like paclitaxel, epothilone B binds to the ??-tubulin heterodimer subunit. Once bound, the rate of ??-tubulin dissociation decreases, thus stabilizing the microtubules.
Furthermore, epothilone B has also been shown to induce tubulin polymerization into microtubules without the presence of GTP. This is caused by formation of microtubule bundles throughout the cytoplasm.
Finally, epothilone B also causes cell cycle arrest at the G2-M transition phase, thus leading to cytotoxicity and eventually cell apoptosis. The ability of epothilone to inhibit spindle function is generally attributed to its suppression of microtubule dynamics but recent studies have demonstrated that suppression of dynamics occurs at concentrations lower than those needed to block mitosis. At the higher antimitotic concentrations, paclitaxel appears to act by suppressing microtubule detachment from centrosomes, a process that is normally activated during mitosis. It is quite possible that epothilone can also act though similar mechanism.
Epothilone b has the most stable microtubule activity making it twice as potent as Epothilone a