Tubulin-IN-63 

Tubulin-IN-63 is a potent tubulin polymerization inhibitor targeting the colchicine-binding site, with an IC₅₀ of 6.03 µM. Tubulin-IN-63 disrupts microtubule dynamics, induces G2/M arrest and apoptosis, thereby suppressing cancer cell proliferation. Tubulin-IN-63 disrupts capillary network formation in human umbilical vein endothelial cells (HUVECs) and exhibits in vivo antitumor efficacy in a B16-F10 mouse model. Tubulin-IN-63 can be used for the research of cancers, such as melanoma, lung cancer, and liver cancer^[1].

Tubulin-IN-63 (compound 4a) (48 h) demonstrates potent antiproliferative activity against multiple cancer cell lines (B16-F10, MCF-7, Hela, and HepG-2) with IC₅₀s of 0.052, 0.045, 0.076, and 0.036 µM, respectively, while showing low cytotoxicity in normal cell lines (HUVECs, MCF-10A, and LO2) with IC₅₀s of 751, 903, and 579 nM, respectively, indicating its selectivity^[1].
Tubulin-IN-63 (48 h) inhibits the proliferation of A549 and A2780 cells with IC₅₀s of 85.3 and 42.4 nM, and retains efficacy against Paclitaxel (HY-B0015)-resistant cells (A549/T and A2780/T cells) with IC₅₀s of 172.5 and 61.8 nM, indicating its capacity to circumvent Paclitaxel-associated drug resistance^[1].
Tubulin-IN-63 (10-100 nM, 24 h) exerts durable inhibition of cancer cell growth and proliferation in HepG-2 cells, as evidenced by a dose-dependent reduction in clonogenic survival after 10-14 days of drug-free culture^[1].
Tubulin-IN-63 (10-100 nM, 48 h) induces G2/M phase cell cycle arrest and apoptosis in HepG-2 cells in a dose-dependent manner^[1].
Tubulin-IN-63 (10-100 nM, 0-24 h) inhibits HepG-2 cell migration in a concentration-dependent manner^[1].
Tubulin-IN-63 (10-100 nM, 12 h) induces dose-dependent microtubule network disruption in HepG-2 cells^[1].
Tubulin-IN-63 (10-100 nM, 6 h) disrupts vascular network formation in HUVECs^[1].

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

Tubulin-IN-63 (compound 4a) (10 mg/kg, i.p., daily for 14 days) significantly inhibits tumor growth in a B16-F10 mouse model, and shows a synergistic effect when combined with PD-L1 inhibitor NP19 (HY-131347)^[1].

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

425.48

C₂₆H₂₃N₃O₃

CN1C=CC2=C1C=CC(C3=CC=C4N=CN=C(C5=CC(OC)=C(OC)C(OC)=C5)C4=C3)=C2

Room temperature in continental US; may vary elsewhere.

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

• [1]. Ren Y, et al. Discovery of novel quinazoline analogs as tubulin inhibitors targeting the colchicine binding site for potent antitumor therapy in combination with PD-L1 inhibitors. Bioorg Chem. Published online November 30, 2025.  [Content Brief]