Tubulin-IN-51 

Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC₅₀ = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models (A549 human non-small cell lung cancer (NSCLC) cells and U87-MG human glioblastoma)^[1].

Tubulin-IN-51 (Compound 8) promotes tubulin polymerization, a phenomenon similar to the effect of paclitaxel, preventes binding of [³H]vinblastine to tubulin^[1].

Tubulin-IN-51 induces apoptosis by downregulating the proportion of cells in the G1 phase at low compound concentrations (10-35 nM) and arrests the G2/M phase at high compound concentrations (35-200 nM), a pattern similar to that observed with paclitaxel^[1].

Tubulin-IN-51 inhibits KB, KB 8.5, and KBV1 Cell Proliferation, with IC₅₀s of 23 nM, 67 nM, 953 nM, respectively^[1].

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

Tubulin-IN-51 (Compound 8) (15-25 mg/kg, i.v., days 0, 7, 14, and 21 after staging) inhibits tumor growth in tumor (A549 human non-small cell lung carcinoma (NSCLC) cells) xenograft mice model^[1].

Tubulin-IN-51 (2.5-50 mg/kg, p.o., days 0, 7 after staging) inhibits tumor growth in tumor (U87-MG human glioblastoma) xenograft mice model^[1].

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

464.82

C₁₈H₁₈ClF₅N₆O

849550-36-3

FC1=CC(OCCCNC)=CC(F)=C1C2=C(N[C@@H](C(F)(F)F)C)N3N=CN=C3N=C2Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhang N, et al. Synthesis and SAR of [1,2,4]triazolo[1,5-a]pyrimidines, a class of anticancer agents with a unique mechanism of tubulin inhibition. J Med Chem. 2007 Jan 25;50(2):319-27.  [Content Brief]