Antiproliferative agent-52 

Antiproliferative agent-52 is a tubulin inhibitor with a porcine tubulin K_D of 29.65 μM. Antiproliferative agent-52 binds to the colchicine-binding site at the α-tubulin and β-tubulin interface and inhibits tubulin polymerization. Antiproliferative agent-52 exhibits antiproliferative activity against tumor cells. Antiproliferative agent-52 serves as a lead compound for development of thienopyrimidine and heterocyclic fused pyrimidines with antiproliferative activity. Antiproliferative agent-52 can be used for the research of ovarian cancer, non-small cell lung cancer^[1].

Antiproliferative agent-52 (compound 4a) (48 h) potently inhibits the proliferation of A549, A2780, SKOV3, and HCC827 human tumor cells with IC₅₀ values ranging from 5.83 to 8.63 nM^[1].
Antiproliferative agent-52 (2-14 h) binds to the colchicine binding site of tubulin within the T2R-TTL complex via hydrophobic interactions, with no hydrogen bonds formed with tubulin residues^[1].
Antiproliferative agent-52 binds directly to purified tubulin with a K_D of 29.65 μM^[1].

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

305.78

C₁₄H₁₂ClN₃OS

2913194-20-2

COC1=CC=C(N(C2=NC(Cl)=NC3=C2SC=C3)C)C=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Wu C, et al. Discovery and mechanistic insights into thieno[3,2-d]pyrimidine and heterocyclic fused pyrimidines inhibitors targeting tubulin for cancer therapy. European Journal of Medicinal Chemistry. 2024;276:116649.