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

529584
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Key Spec Table

Empirical FormulaCAS #
C₁₇H₁₇N₇ 1092788-83-4

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529584-5MGCN
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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, mTOR Inhibitor VII, PI 3-K Inhibitor XIII, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII, 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
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      PTK/PI 3-K/mTOR Inhibitor, PP121 - CAS 1092788-83-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      529584

      References

      Reference overview
      Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision25-May-2011 RFH
      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, mTOR Inhibitor VII, PI 3-K Inhibitor XIII, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PDGFR Tyrosine Kinase Inhibitor XVIII, Abl Inhibitor IV
      DescriptionA 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.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1092788-83-4
      Chemical formulaC₁₇H₁₇N₇
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      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.
      Toxicity Standard Handling
      ReferencesApsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.