Tubulin degrader 1 

Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC₅₀ values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth^[1].

Tubulin degrader 1 (0.2-25 μM, 24 h) exerts its antiproliferative activity by directly binding to the colchicine-site in Hela cells^[1].
Tubulin degrader 1 (0-300 nM, 24 h) can cause apparent G2/M phase cell cycle arrest and cell apoptosis in A2780S and A2780T cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tubulin degrader 1 (10-30 mg/kg, i.v., every two days for 6-9 doses) has antitumor activity in A2780S and A2780T xenograft models^[1].

Pharmacokinetic Analysis in Male Sprague–Dawley Rat Model^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

345.40

C₂₀H₁₉N₅O

COC1=CC=CC(C2=CC(NCC3=CC4=C(NC=C4)C=C3)=NC(N)=N2)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhang C, et al. Structure-based design and synthesis of BML284 derivatives: A novel class of colchicine-site noncovalent tubulin degradation agents. Eur J Med Chem. 2024 Feb 27;268:116265.  [Content Brief]