538759 MCT1 Inhibitor III - Calbiochem

538759
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₁₇N₂NaO₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38759.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC50 = 11 nM for [14C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L; 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 61.333 mg/L).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number538759
          Brand Family Calbiochem®
          Synonyms(E)-2-Cyano-3-(4-(diphenylamino)-2-methoxyphenyl)acrylate, Sodium, Monocarboxylate Transport 1 Inhibitor III
          DescriptionMCT1 Inhibitor III
          References
          ReferencesGurrapu, S., et al. 2015. ACS Med. Chem. Lett. 6, 558.
          Product Information
          FormYellow solid
          Hill FormulaC₂₃H₁₇N₂NaO₃
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          Biological Information
          Primary TargetMCT1
          Primary Target IC<sub>50</sub>11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4
          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 -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          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

          MCT1 Inhibitor III - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Gurrapu, S., et al. 2015. ACS Med. Chem. Lett. 6, 558.
          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.

          Revision19-November-2016 JSW
          Synonyms(E)-2-Cyano-3-(4-(diphenylamino)-2-methoxyphenyl)acrylate, Sodium, Monocarboxylate Transport 1 Inhibitor III
          DescriptionA cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC50 = 11 nM for [14C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L; 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 61.333 mg/L).
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°C
          Hygroscopic
          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
          ReferencesGurrapu, S., et al. 2015. ACS Med. Chem. Lett. 6, 558.