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538759 MCT1 Inhibitor III - Calbiochem

A water-soluble, bioavailable, nontoxic, potent & reversible MCT1 inhibitor (IC₅₀ = 11 nM). Efficiently suppresses colorectal adenocarcinoma xenograft tumor growth in mouse model (i.p. & p.o.).

MCT1 Inhibitor III - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (E)-2-Cyano-3-(4-(diphenylamino)-2-methoxyphenyl)acrylate, Sodium, Monocarboxylate Transport 1 Inhibitor III

Primary Target: MCT1
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538759
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₁₇N₂NaO₃

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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.38759.0001 04054839119637

      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 Protect from light
      -20°C
      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.
      Toxicity Standard Handling
      ReferencesGurrapu, S., et al. 2015. ACS Med. Chem. Lett. 6, 558.