SW-106065

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SW-106065 是 MPNST（恶性周围神经鞘瘤）细胞凋亡的新型药理学诱导剂。

SW-106065 is a novel pharmacologic inducer of apoptosis in MPNST (malignant peripheral nerve sheath tumors); inhibits ATP consumption of sMPNST and other models of MPNST with EC50 of 1 uM, shows no toxicity to normally dividing Schwann cells or mouse embryonic fibroblasts; reduces MPNST burden in a mouse allograft model.

SW106065 (Compound 21, Cpd21) inhibits the human MPNST cell lines growth in a dose-dependent manner, and EC50 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 μMIncubation Time:24 hoursResult:Decreased levels of Cyclin D1 protein.

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 | MPNST-IN-21

Apoptosis

Apoptosis

Apoptosis

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62289-81-0

204.247

C10H8N2OS

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (489.60 mM)

C1=CC(=CN=C1)NC(=O)C2=CC=CS2

N-(pyridin-3-yl)thiophene-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years