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SP-141

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

inhibit|degradation|auto-ubiquitination|cancer|breast|SP 141|SP141|SP-141|pancreatic|Inhibitor|Mdm2|MDM-2/p53

验证数据展示

  • CAS No.: 1253491-42-7

    SP-141
    CAS#: 1253491-42-7

产品信息

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 98.01%， 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 | Shipping with blue ice.
别名 inhibit|degradation|auto-ubiquitination|cancer|breast|SP 141|SP141|SP-141|pancreatic|Inhibitor|Mdm2|MDM-2/p53

体内活性

向裸鼠注射SP141（40 mg/kg/d）能显著抑制异种移植瘤的生长（与对照组相比减少了75%），并导致原位肿瘤的退缩[1]。

体外活性

SP141直接与MDM2结合，促进其自身泛素化和通过蛋白酶体的降解。该化合物降低了胰腺癌细胞系中MDM2的水平及其增殖率，50%抑制浓度<0.5 μM（0.38-0.50 μM）。SP141浓度的增加导致胰腺癌细胞系中凋亡水平和G2-M期阻滞的增加，无论它们是否表达功能性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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