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Tubulin degrader 1 (Compound 5i), a derivative of BML284, is an orally active non-covalent microtubule protein degrader targeting the colchicine site. It exhibits IC50 values ranging from 0.02 to 0.05 μM across five tumor cell lines (Hela, HCT116, MCF-7, K562, and Molm-13). Tubulin degrader 1 demonstrates antiproliferative properties and effectively inhibits tumor growth.
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| 10 mg | Inquiry | Backorder | Backorder | |
| 50 mg | Inquiry | Backorder | Backorder |
| Description | Tubulin degrader 1 (Compound 5i), a derivative of BML284, is an orally active non-covalent microtubule protein degrader targeting the colchicine site. It exhibits IC50 values ranging from 0.02 to 0.05 μM across five tumor cell lines (Hela, HCT116, MCF-7, K562, and Molm-13). Tubulin degrader 1 demonstrates antiproliferative properties and effectively inhibits tumor growth. |
| In vitro | Tubulin degrader 1, when used at concentrations of 0.2-25 μM for 24 hours, exhibits antiproliferative activity by directly binding to the colchicine site in Hela cells. At 0-300 nM for 24 hours, it can induce significant G2/M phase cell cycle arrest and apoptosis in A2780S and A2780T cells. |
| In vivo | Tubulin degrader 1, administered intravenously at a dosage of 10-30 mg/kg every other day for a total of 6-9 doses, exhibits antitumor activity in A2780S and A2780T xenograft models. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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