Bioactivity | Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor with an IC50 of 3.15 μM. Tubulin polymerization-IN-14 shows potent anti-vascular and anticancer activities, induces cancer cell apoptosis[1]. |
Target | IC50: 3.15 μM (tubulin polymerization) |
Invitro | Tubulin polymerization-IN-14 (Compound 20a) binds to the colchicine binding site on tubulin[1].Tubulin polymerization-IN-14 (0-1 μM; 72 h) inhibits cancer cell growth[1].Tubulin polymerization-IN-14 (5-20 nM; 48 h) arrests K562 cell cycle at G2/M phase, significantly induces cell apoptosis in K562 cells in a concentration-dependent manner, and induces mitochondrial membrane potential (MMP) collapse and mitochondrial dysfunction in K562 cells[1].Tubulin polymerization-IN-14 (5-20 nM; 24 h) significantly decreases wound closure and capillary-like tubules formation in a concentration-dependent manner in HUVECs[1]. Cell Proliferation Assay[1] Cell Line: |
In Vivo | Tubulin polymerization-IN-14 (Compound 20a) (15 and 30 mg/kg; i.v.; daily for 21 days) displays obvious and dose-dependent antitumor effect with no significant toxicity in the liver tumor allograft mouse model[1]. Animal Model: |
Name | Tubulin polymerization-IN-14 |
CAS | 2417134-05-3 |
Formula | C15H15ClN2O2 |
Molar Mass | 290.74 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Shuai W, et al. Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors. Eur J Med Chem. 2020 Jul 1;197:112308. |