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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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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₁₇N₂NaO₃

Products

Catalogue NumberPackaging Qty/Pack
5.38759.0001 Glass bottle 10 mg
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.