Tubulysin A

Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC₅₀ values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin^[1][2][3][4]. In Vitro:The IC₅₀ values of Tubulysin A in the NCI-H1299 (lung), HT-29 (colon) and A2780 (ovary) cell lines are 3, 1 and 2 nmol/L, respectively^[4].
The IC₅₀ values of Tubulysin A against L929 (mouse fibroblast) and KB-V1 (human cervical cancer multidrug resistant cell line) cells were 0.07 and 1.4 ng/ml, respectively^[1].
Tubulysin A (1 nM, 10 nM; 24h) has an antiangiogenic effect in HUVEC cells with IC₅₀ values of 2.07-2.97 nM^[1].
Tubulysin A (5h) can inhibit cell migration in HUVEC cells with IC₅₀ value of 2.26 nM^[1].
Tubulysin A (72h) can inhibit cell growth in HUVEC cells with GI₅₀ value of 0.34 nM^[1].
In Vivo:Tubulysin A (0.04 mg/kg, 0.06 mg/kg; Intraperitoneal (i.p.); once daily for 4 days) can inhibit the growth of tumor cells in mouse xenotransplantation model^[1].