PP121

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Chemical Structure| 1092788-83-4 同义名 : -
CAS号 : 1092788-83-4
货号 : A986976
分子式 : C17H17N7
纯度 : 99%+
分子量 : 319.36
MDL号 : MFCD12912434
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(56.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • mTOR

    mTOR, IC50:13 nM

  • DNA-PK

    DNA-PK, IC50:60 nM

  • PDGFR

    PDGFR, IC50:2 nM

  • Src

    Src, IC50:14 nM

  • Abl

    Abl, IC50:18 nM
描述 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.66mL

3.13mL

1.57mL

31.31mL

6.26mL

3.13mL
参考文献

[1]Peng Y, Zhou Y, et al. The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44.

[2]Apsel B, Blair JA, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.