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Pro-905 是一种具有抗肿瘤活性的亚磷酸盐肽。Pro-905 将活性核苷酸抗代谢物硫代鸟苷单磷酸(TGMP) 递送到肿瘤。Pro-905 能有效阻止嘌呤残留底物与核酸的结合,抑制人类恶性周围神经鞘肿瘤 (MPNST) 细胞的集落形成。 Pro-905 抑制嘌呤残留进入核酸并阻止细胞生长。 Pro-905 抑制 MPNST 的生长,增强 JHU395 (HY-124778) 的抗肿瘤作用。

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PRO-905 Chemical Structure

PRO-905 Chemical Structure

CAS No. : 2762209-68-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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) [1].

体外研究
(In Vitro)

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 [1]
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[1]
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[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: sNF96.2 and JH-2-002 human MPNST cells
Concentration: 10 µM (in combination with JHU395 (HY-124778)(1µM))
Incubation Time: 120 h
Result: Inhibited cell proliferation with effects on nucleic acid and induced DNA damage (γH2AX).
体内研究
(In Vivo)

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[1]
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[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B6 mice with flank MPNST[1]
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 [1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection
Result: Caused animal body weights remained within 10% of starting weights over two weeks of dosing.
分子量

568.54

Formula

C22H29N6O8PS

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PRO-905
目录号:
HY-155995
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