CTCE 9908 acetate is an antagonist of CXCR4 and inhibits migration in CXCR4-expressing ovarian cancer cells.

CTCE 9908 acetate inhibited ovarian cancer cell migration to CXCL12, but on longer incubation, caused cell death in CXCR4-positive cells. CTCE 9908 acetate did not cause apoptosis or cellular senescence, but induced multinucleation, G(2)-M arrest, and abnormal mitosis in ovarian cancer cells. CTCE 9908 acetate deregulated DNA damage checkpoint proteins and spindle assembly checkpoint proteins at G(2)-M phases of the cell cycle. Combination treatment of CTCE 9908 acetate and the drug paclitaxel led to an additive cytotoxicity that also involved mitotic catastrophe[1].

In dosing experiment of CTCE 9908 acetate in the PyMT mouse model, increasing doses of CTCE 9908 acetate alone slowed the rate of tumor growth, with a 45% inhibition of primary tumor growth at 3.5 weeks of treatment with 50 mg/kg of CTCE 9908 acetate (p = 0.005). Expression levels of VEGF were also found to be reduced by 42% with CTCE 9908 acetate (p = 0.01). In combination with docetaxel, CTCE 9908 acetate administration decreased tumor volume by 38% (p = 0.02), an effect that was greater than that observed with docetaxel alone. In combination with DC101, CTCE 9908 acetate also demonstrated an enhanced effect compared to DC101 alone, with a 37% decrease in primary tumor volume (p = 0.01) and a 75% reduction in distant metastasis (p = 0.009). In combination with docetaxel or an anti-angiogenic agent, the anti-tumor and anti-metastatic effects of CTCE 9908 acetate were markedly enhanced[2].