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Epothilone A 152044-53-6

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Synonyms
Appearance
Chemical Formula
C26H39NO6S
Solubility
Molecular Weight
493.66
Storage and Stability
in stock
CAS No.
152044-53-6
Purity
98%+
Introduction
Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM.


Epothilone A, discovered from the myxobacterium Sorangium cellulosum, is a Taxol-like microtubule-stabilizing agent that induces tubulin polymerization, leading to cell cycle arrest at the G2-M transition, cytotoxicity, and apoptosis. Epothilone A potently inhibits cell proliferation in HCT116 cells, with IC50 of 4.4 nM. [1] Epothilone A also displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 values ranging from 13 nM to 160 nM. Epothilone A is more water soluble than Taxol and competes with Taxol in binding with microtubules, with IC50 of 2.3 μM. [2] However, both Epothilone A and Taxol don't share a common pharmacophore and exploits the tubulin-binding pocket uniquely and independently. [3] Recently, it is found that microbiological transformation of Epothilone A by Aspergillus niger AS 3.739 yields several metabolites that is also toxic to MCF-7 cells, but with much higher IC50 values. [4]
 

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