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529584 PTK/PI 3-K/mTOR Inhibitor, PP121 - CAS 1092788-83-4 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1092788-83-4C₁₇H₁₇N₇

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529584-5MG
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      Description
      OverviewA cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50 <0.26 µM against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, SrcT338I, and VEGFR2) and PI 3-K family kinases (IC50 <1.4 µM against p110α/ β/ δ/ γ, mTOR, and DNA-PK). PP121 is less effective against ser/thr kinases and exhibits significant inhibition of only 14 ser/thr kinases (≥70% inhibition with 1 µM inhibitor and 10 µM ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI 3-K/mTOR pathway by PI-103 (IC50 = 800 nM, Cat. Nos. 528100 and 528101) is shown to be less effective than PP121 treatment (IC50 = 50 nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.
      Catalogue Number529584
      Brand Family Calbiochem®
      Synonyms1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, PI 3-K Inhibitor XIII, mTOR Inhibitor VII, Abl Inhibitor IV, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII
      References
      ReferencesApsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.
      Product Information
      CAS number1092788-83-4
      FormWhite solid
      Hill FormulaC₁₇H₁₇N₇
      Chemical formulaC₁₇H₁₇N₇
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥98% by HPLC
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      529584-5MG 04055977269901