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

529584
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₇N₇ 1092788-83-4

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      529584-5MG
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          5 mg
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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
          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 SDS

          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.