Epothilone B

SKU: orb1301096

Description

Epothilone B (Patupilone) is a microtubule-stabilizing agent isolated from Sorangium cellulosum. Unlike taxanes, it retains cytotoxicity against P-glycoprotein-overexpressing multidrug-resistant cells. It is widely used in cancer research, demonstrating antitumor activity in both in vitro cytotoxicity assays and in vivo xenograft models.

Research Area

Cell Biology, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 152044-54-7
• MW: 507.68
• Purity: 99.84% (May vary between batches)
• Formula: C₂₇H₄₁NO₆S
• SMILES: C[C@H]1CCC[C@@]2(C)O[C@H]2C[C@H](OC(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@H]1O)C(\C)=C\c1csc(C)n1
• Target: Apoptosis,Antibacterial,Microtubule Associated,Antibiotic,Antifungal
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.97 mM);DMSO:5.1 mg/mL (10.05 mM)

Bioactivity

• Target IC50:
  Tubulin:1.8 μM(EC0.01)
• In Vivo:
  In a mouse xenograft model of RPMI 8226 cells, Epothilone B (2.5 mg/kg–4 mg/kg) prolongs survival and suppresses tumor growth. Similarly, in mouse xenograft models of prostate cancer cells, including DU145 and PC3, Epothilone B at the same dose also inhibits tumor growth.
• In Vitro:
  Epothilone B shows better activity than Epothilone A. The EC0.01 of Epothilone B is 1.8 μM. Epothilone B potently inhibits cell proliferation in HCT116 cells, with IC50 of 0.8 nM. Epothilone B induces mitotic arrest and displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 of 3 nM to 92 nM. Epothilone B competes with Taxol in binding to microtubules, with IC50 of 3.3 μM. In MCF-7 cells overexpressing GFP-α-tubulin, Epothilone B (3.5 nM) efficiently blocks microtubule dynamics. Meanwhile, Epothilone B induces mitotic arrest with IC50 of 3.5 nM. In multiple myeloma (MM) cells, including RPMI 8226, U266, MM.1S, LR5, and MR20, Epothilone B directly suppresses proliferation with IC50 of 1 nM to 10 nM. Similarly, Epothilone B (10 nM) also induces cell cycle arrest and apoptosis. A recent study reveals that, in ovarian cancer Hey cells, Epothilone B (5 nM–100 nM) enhances surface epithelial cell adhesion antigen (EpCAM), without affecting the transcription or the total cellular level of EpCAM.
• Cell Research:
  For mitotic block and aberrant mitosis, cells are plated either in 48-well plates (for trypan blue and cell counting) or onto coverslips. After 24 hours, cells are treated with Epothilone B and scored at regular intervals. For the cytotoxicity analysis, cells are counted and scored as trypan blue positive or negative. Concurrently, coverslips andaliquots of cells in the culture supernatant are fixed and stained with Hoechst33342 in PBS. These cells are scored for cells blocked at the G2/M transition and aberrant mitosis.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Antibiotic, Apoptosis, inhibit, Microtubule/Tubulin, Microtubule Associated, MicrotubuleAssociated, Patupilone, Inhibitor, Fungal, Epothilone B, EPO 906, EPO906, EPO-906, Tubulin

Compound Identifiers

PubChem CID

448013