PROTAC tubulin-Degrader-1 

PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056))^[1].

PROTAC tubulin-Degrader-1 (Compound W13) (4-21 nM, 72 h) exhibits potent antiproliferative activity against multiple human tumor cell lines (MCF-7, A549, HepG2, MGC-803, HeLa, U937), with IC₅₀ values ranging from 0.004 μM to 0.021 μM^[1].
PROTAC tubulin-Degrader-1 (0-1.25 μM, 48 h) effectively degrades α-tubulin (DC₅₀ = 296 nM in A549, DC₅₀ = 32 nM in A549/Taxol), β-tubulin (DC₅₀ = 856 nM in A549, DC₅₀ = 972 nM in A549/Taxol) and potently degrades β3-tubulin (DC₅₀ = 251 nM in A549, DC₅₀ = 5 nM in A549/Taxol) in A549 and A549/Taxol cells^[1].
PROTAC tubulin-Degrader-1 (0.25 μM, 24-48 h) induces tubulin degradation via the ubiquitin-proteasome system (UPS)^[1].
PROTAC tubulin-Degrader-1 (2-50 nM, 24-48 h) induces G2/M phase arrest and promotes apoptosis in A549 and A549/Taxol cells in a dose-dependent manner^[1].
PROTAC tubulin-Degrader-1 (2-50 nM, 14 days) inhibits colony formation of A549 and A549/Taxol cells in a dose-dependent manner^[1].
PROTAC tubulin-Degrader-1 (2.5-10 nM, 6-8 h) strongly inhibits tube formation of human umbilical vein endothelial cells (HUVECs) on Matrigel, reducing the number of nodes, master junctions, segments length, total branching length and meshes in a dose-dependent manner^[1].

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

PROTAC tubulin-Degrader-1 (Compound W13) (15 mg/kg, i.p., once every two days, 23 days) demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model^[1].

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

657.67

C₃₅H₃₅N₃O₁₀

COC1=C(OC)C(OC)=CC(/C=C\C2=CC=C(OC)C(OC(CCCN3C(CCC(N4C(C(C(N)=CC=C5)=C5C4=O)=O)C3=O)=O)=O)=C2)=C1

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

• [1]. Yang H, et al.Discovery of the cereblon-recruiting tubulin PROTACs effective in overcoming Taxol resistance in vitro and in vivo. Eur J Med Chem. 2023 Dec 27;265:116067.  [Content Brief]