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SP-141

SP-141 是一种 MDM2 抑制剂，可促进 MDM2 自身泛素化和降解，具有抗癌活性。

CAS号

1253491-42-7

分子式

C22H16N2O

主要靶点

Mdm2

仅限科研使用

Cat No : CM05046

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Synonyms

SP 141

验证数据展示

  • CAS No.: 1253491-42-7

    SP-141
    CAS#: 1253491-42-7

产品信息

SP 141 is a MDM2 inhibitor.SP-141 promotes MDM2 auto-ubiquitination and degradation, with anticancer activity.

CAS号 1253491-42-7
分子式 C22H16N2O
主要靶点 Mdm2
主要通路 凋亡
分子量 324.38
纯度 99.21%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 SP 141

体内活性

Injection of nude mice with SP141 (40 mg/kg/d) inhibited growth of xenograft tumors (by 75% compared with control mice), and led to regression of orthotopic tumors[1].

体外活性

SP141, which bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome.?The compound reduced levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation, with 50% inhibitory concentrations <0.5 μM (0.38-0.50 μM).?Increasing concentrations of SP141 induced increasing levels of apoptosis and G2-M-phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53[1].

溶解度

DMSO:4.4 mg/mL (13.56 mM)

参考文献

1.Wei Wang, et al. The Pyrido[b]indole MDM2 Inhibitor SP-141 Exerts Potent Therapeutic Effects in Breast Cancer Models. Nat Commun. 2014 Oct 1;5:5086.
2.Wei Wang , et al. Identification of a New Class of MDM2 Inhibitor That Inhibits Growth of Orthotopic Pancreatic Tumors in Mice. Gastroenterology. 2014 Oct;147(4):893-902.e2.

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The dilution calculator equation

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