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

The PTK/PI 3-K/mTOR Inhibitor, PP121, also referenced under CAS 1092788-83-4, controls the biological activity of PTK/PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation &

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Synonyms: 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII, mTOR Inhibitor VII, PI 3-K Inhibitor XIII, Abl Inhibitor IV

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529584
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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, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII, mTOR Inhibitor VII, PI 3-K Inhibitor XIII, Abl Inhibitor IV
      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