524619 | PIP3 Antagonist II, DM-PIT-1 - CAS 701947-53-7 - Calbiochem

524619
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₆H₁₅N₃O₄S 701947-53-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      524619-25MG
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable benzoylthiourea compound that is shown to compete against PIP3 (Cat. No. 524615) for binding PH domains of Akt1 (IC50 ≥31 µM), ARNO, GRP1, and PKD1. Effectively blocks PIP3-dependent cellular PI3K-PDK1-Akt signaling pathway activation in U87MG (25 to 100 µM for 3 d) and PDGF-induced Akt and GRP membrane translocation in serum-starved SUM159 cells (1 h 100 µM pretreatment), while being inactive against PDGF-induced Btk translocation or PMA-induced PLC-δ and TAPP1/2 translocations. Although DM-PIT-1 can be administered as a DMSO stock for effective culture treatments, incorporating DM-PIT-1 into PEG-PE mixed micelles enhances its solubility (up to 1 mM) and i.v. dosing limit for more effective in vivo administrations (5% vs. 41% of control 4T1 tumor size in mice via 1 mg/kg micelles-formulated or 0.4 mg/kg free drug daily i.v., respectively).
          Catalogue Number524619
          Brand Family Calbiochem®
          SynonymsN-​(((2-Hydroxy-​5-​nitrophenyl)amino)thioxomethyl)-​3,​5-​dimethyl-​benzamide, N-((2-Hydroxy-5-nitrophenyl)carbamothioyl)-3,5-dimethylbenzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI
          References
          ReferencesMiao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
          Skidan, I., et al. 2009. Drug Deliv. 16, 45.
          Product Information
          CAS number701947-53-7
          FormOff-white powder
          Hill FormulaC₁₆H₁₅N₃O₄S
          Chemical formulaC₁₆H₁₅N₃O₄S
          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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Regulatory Review
          Storage +2°C to +8°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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          524619

          References

          Reference overview
          Miao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
          Skidan, I., et al. 2009. Drug Deliv. 16, 45.
          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.

          Revision17-July-2012 JSW
          SynonymsN-​(((2-Hydroxy-​5-​nitrophenyl)amino)thioxomethyl)-​3,​5-​dimethyl-​benzamide, N-((2-Hydroxy-5-nitrophenyl)carbamothioyl)-3,5-dimethylbenzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI
          DescriptionA cell-permeable benzoylthiourea compound that is shown to compete against PIP3 (Cat. No. 524615) for binding PH (pleckstrin-homology) domains of Akt1 (IC50 ≥31 µM using recombinant human Akt1 aa 1-123), ARNO, GRP1, and PKD1, while lacking activity against PIP3 Btk PH domain ineraction, PI-4,5-P2 (Cat. Nos. 524614, 524644, and 524646) PLC-δ PH domain binding, or PI-3,4-P2 TAPP1/2 PH domains binding, resulting in effective blockage of PIP3-dependent PI3K-PDK1-Akt signaling pathway activation in human glioblastoma U87MG cultures (25 to 100 µM for 3 d) and (5 min 100 ng/ml) PDGF-induced Akt and GRP membrane translocation (by 85% and 70%, respectively, with 1 h 100 µM pretreatment) in serum-starved human breast cancer SUM159 cells, while being inactive against PDGF-induced Btk translocation or (5 min 250 ng/ml) PMA-induced PLC-δ and TAPP1/2 translocations. Although DM-PIT-1 can be administered as a DMSO stock for effective culture treatments, incorporating DM-PIT-1 into PEG-PE mixed micelles is reported to enhance its solubility (up to 1 mM), and presumably delivery efficiency (57% vs. 67% U87MG viability after 24 h 50 µM drug treatment, respectively, with or without PEG-PE encapsulation), making large dosage delivery possible for more effective in vivo administrations (5% vs. 41% of control 4T1 tumor size in mice after 8 daily i.v. dosages of 1 mg/kg micelles-formulated or 0.4 mg/kg free drug, respectively).
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number701947-53-7
          Chemical formulaC₁₆H₁₅N₃O₄S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (25 mg/ml)
          Storage +2°C to +8°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 Regulatory Review
          ReferencesMiao, B., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 20126.
          Skidan, I., et al. 2009. Drug Deliv. 16, 45.