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编 号：F762667
分子式：C22H29N6O8PS
分子量：568.54
分子式：C22H29N6O8PS
分子量：568.54
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CAS No: 2762209-68-5
产品详情
生物活性：
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
体内研究：
Pro-905 (20 mg/kg, 腹腔注射, 每周5天给药, 持续4周) 在携带人 MPNST PDX JH-2-031 的 NSG 小鼠模型中减缓了肿瘤的生长。Pro-905 (10 mg/kg, 腹腔注射, 一周5天给药) 与 JHU395 (1.2 mg/kg, p.o.) 联合用药在 B6 翼侧 MPNST 小鼠模型中抑制肿瘤核苷酸代谢，抑制 MPNST 增殖。Animal Model:B6 mice with flank MPNST
Dosage:10 mg/kg (in combination with JHU3955 (1.2 mg/kg, p.o.))
Administration:Intraperitoneal injection
Result:Prevented growth of established tumors to a greater extent.Induced tumors significantly decrease, mean percent proliferation, JHU395 0.82%, Pro-905 1.25%, combination 0.18%.
Animal Model:Nod scid gamma (NSG) mice with JH-2-031 MPNST
Dosage:20 mg/kg
Administration:Intraperitoneal injection
Result:Caused animal body weights remained within 10% of starting weights over two weeks of dosing.
体外研究：
Pro-905 (10 μM, 120 h) 与JHU395 (1 μM, 120 h) 联合用药抑制 JH-2-002 细胞增殖和鸟嘌呤并入新合成的 DNA 和 RNA 。Pro-905 (10 μM, 120 h) 与 JHU395 (1 μM, 120 h) 联合用药可抑制 sNF96.2 和 JH-2-002 人 MPNST 细胞的集落形成。Pro-905 (10 μM, 6 h) 在 sNF96.2 细胞中对嘌呤依赖性 3H-次黄嘌呤与 DNA 和 RNA 的结合有抑制作用。
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
体内研究：
Pro-905 (20 mg/kg, 腹腔注射, 每周5天给药, 持续4周) 在携带人 MPNST PDX JH-2-031 的 NSG 小鼠模型中减缓了肿瘤的生长。Pro-905 (10 mg/kg, 腹腔注射, 一周5天给药) 与 JHU395 (1.2 mg/kg, p.o.) 联合用药在 B6 翼侧 MPNST 小鼠模型中抑制肿瘤核苷酸代谢，抑制 MPNST 增殖。Animal Model:B6 mice with flank MPNST
Dosage:10 mg/kg (in combination with JHU3955 (1.2 mg/kg, p.o.))
Administration:Intraperitoneal injection
Result:Prevented growth of established tumors to a greater extent.Induced tumors significantly decrease, mean percent proliferation, JHU395 0.82%, Pro-905 1.25%, combination 0.18%.
Animal Model:Nod scid gamma (NSG) mice with JH-2-031 MPNST
Dosage:20 mg/kg
Administration:Intraperitoneal injection
Result:Caused animal body weights remained within 10% of starting weights over two weeks of dosing.
体外研究：
Pro-905 (10 μM, 120 h) 与JHU395 (1 μM, 120 h) 联合用药抑制 JH-2-002 细胞增殖和鸟嘌呤并入新合成的 DNA 和 RNA 。Pro-905 (10 μM, 120 h) 与 JHU395 (1 μM, 120 h) 联合用药可抑制 sNF96.2 和 JH-2-002 人 MPNST 细胞的集落形成。Pro-905 (10 μM, 6 h) 在 sNF96.2 细胞中对嘌呤依赖性 3H-次黄嘌呤与 DNA 和 RNA 的结合有抑制作用。
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