SW106065 (Cpd21; 40 mg/kg; intraperitoneal injection; twice per day for 4 weeks) treatment can be delivered to mice in concentrations to sufficiently penetrate sMPNST tissue, and inhibit tumor development. Animal Model: NCR-nu/nu female mice (6-7 week old) injected with MPNST cells Dosage: 40 mg/kg Administration: Intraperitoneal injection; twice per day for 4 weeks Result: Reduced MPNST burden in a mouse allograft model.

SW106065 (Compound 21, Cpd21) inhibits the human MPNST cell lines growth in a dose-dependent manner, and EC 50 concentrations of 439 nM and 753.6 nM for S462 and SNF96.2 cells, respectively. SW106065 remains nontoxic to normally dividing Schwann cells or mouse embryonic fibroblasts. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment shows a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. And increases levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner. SW106065 (Cpd21; 0.25-5 µM; 24 hours; sMPNST cells) treatment decreases the levels of Cyclin D1 protein. SW106065 (Cpd21) treatment significant increase in the percentage of apoptotic cells. Cell Cycle Analysis Cell Line: sMPNST cells Concentration: 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM Incubation Time: 24 hours Result: Showed a decreased percentage of cells in S phase, and a corresponding increased percentage in G1/G0 and G2/M. RT-PCR Cell Line: sMPNST cells Concentration: 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM Incubation Time: 24 hours Result: Decreased levels of cyclin A2, cyclin B1, cyclin D1, cyclin E, cdk4, and cdk6. Increased levels of cdkn1a and cdkn2a mRNA were observed in a dose-dependent manner. Western Blot Analysis Cell Line: sMPNST cells Concentration: 0.25 µM, 0.5 µM, 1 µM, 2.5 µM, and 5 µM Incubation Time: 24 hours Result: Decreased levels of Cyclin D1 protein.

SW106065 是恶性周围神经鞘瘤 (MPNST) 的凋亡 (apoptosis) 诱导剂。SW106065 以 EC50 为 1 µM 来抑制 sMPNST 细胞和其他模型中 MPNST 的 ATP 消耗。SW106065 可用于 MPNST 的研究。