531005 PFKFB3 Inhibitor II, PFK15 - Calbiochem

531005
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₂N₂O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31005.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC50 = 207 nM compared to 22.9 µM for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 µM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 µM. Induces apoptosis and reduces proliferation in transformed cells (mean GI50 of ~3 µM in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531005
          Brand Family Calbiochem®
          Synonyms(E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, PFK15
          References
          ReferencesClem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461.
          Product Information
          FormLight beige solid
          Hill FormulaC₁₇H₁₂N₂O
          Chemical formulaC₁₇H₁₂N₂O
          ReversibleY
          Applications
          Biological Information
          Primary TargetPFKFB3
          Primary Target IC<sub>50</sub>207 nM for hrPFKFP3
          Purity≥97% 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 (-70°C). Stock solutions are stable for up to 6 months at -70°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          PFKFB3 Inhibitor II, PFK15 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Clem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461.
          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.

          Revision15-August-2014 JSW
          Synonyms(E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, PFK15
          DescriptionA cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC50 = 207 nM compared to 22.9 µM for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 µM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 µM. Induces apoptosis and reduces proliferation in transformed cells (mean GI50 of ~3 µM in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).
          FormLight beige solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₁₂N₂O
          Purity≥97% by HPLC
          SolubilityDMSO (10 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
          Toxicity Standard Handling
          ReferencesClem, B. F., et al. 2013. Mol. Cancer Ther. 12, 1461.