128125 Aloisine A - CAS 496864-16-5 - Calbiochem

128125
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₁₆H₁₇N₃O496864-16-5

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      US1128125-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM and 1.5 µM for GSK-3α, GSK-3β, respectively), and c-Jun N-terminal kinase (JNK; IC50 = ~ 3 - 10 µM). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC50 ≥ 100 µM). Shown to arrest cells in both G1 and G2 phases (IC50 = 7 µM and 10.5 µM for undifferentiated human teratocarcinoma cells NT2 and differentiated postmitotic neurons hNT, respectively). Shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively).
          Catalogue Number128125
          Brand Family Calbiochem®
          SynonymsRP107, 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
          References
          ReferencesNoel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
          Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.
          Product Information
          CAS number496864-16-5
          ATP CompetitiveY
          FormYellow solid
          Hill FormulaC₁₆H₁₇N₃O
          Chemical formulaC₁₆H₁₇N₃O
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetCyclin-dependent kinases
          Primary Target IC<sub>50</sub>150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively; 500 nM and 1.5 µM for GSK-3α, GSK-3β, respectively
          Primary Target K<sub>i</sub>EC50 = 150 nM, 140 nM and 111 nM, in stimulating CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM Forskolin, respectively
          Purity≥95% by HPLC
          Physicochemical Information
          Cell permeableY
          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 +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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Certificates of Analysis

          TitleLot Number
          128125

          References

          Reference overview
          Noel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
          Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.

          Brochure

          Title
          Alzheimer's Disease Brochure & Technical Guide
          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.

          Revision13-December-2007 JSW
          SynonymsRP107, 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
          DescriptionA cell-permeable, pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM for Cdk1/cyclin B, 120 nM for Cdk2/cyclin A, 400 nM for Cdk2/cyclin E, and 160 nM for Cdk5/p25), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM for GSK-3α and 1.5 µM for GSK-3β), and c-Jun N-terminal kinase (JNK; IC50 ~3-10 µM). Also inhibits extracellular signal-regulated kinases (ERKs; IC50 = 18 µM for ERK1 and 22 µM for ERK2), PIM1 (IC50 > 10 µM), and insulin receptor tyrosine kinase (IC50 = 60 µM) at higher concentrations. Does not significantly inhibit Cdk4/cyclin D1, CK1, CK2, MAPKK, PKA, PKG, PKCs, or c-raf (IC50 = ≥ 100 µM). Shown to arrest undifferentiated human teratocarcinoma cells (NT2) and differentiated post-mitotic neurons (hNT) in both G1 and G2 phases (IC50 = 7 µM and 10.5 µM, respectively). Also shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM of Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively).
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number496864-16-5
          Chemical formulaC₁₆H₁₇N₃O
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (10 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesNoel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
          Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.