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509663 MCT1 Inhibitor, SR13800 - CAS 227321-12-2 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
227321-12-2C₂₅H₂₉N₃O₂S

Products

Catalog NumberPackaging Qty/Pack
5.09663.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable pyrole pyrimidine-based compound that acts as an inhibitor of monocarboxylate transporter 1 (MCT1, SLC16A1) and blocks the proliferation of Raji Burkitt lymphoma (Raji BL) cells expressing MCT1 (EC50 = 5 nM). Also shown to inhibit the growth of MCF-7 breast cancer cells. Effectively increases intracellular lactate levels while reducing lactate export and intracellular ATP levels in Raji cells. However, it does not affect basal oxygen consumption or the mitochondrial mass in these cells. Delays or even eliminates tumor growth in NOD/SCID mice injected with Raji lymphoma cells. Acts synergistically with metformin (Cat. No. 317240) to block monocarboxylate transport and tumor growth in humans and in murine models. Their combined effect also reduces cellular levels of glutathione with concomitant increase in hydrogen peroxide levels, which increases the death of Raji BL cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number509663
Brand Family Calbiochem®
SynonymsMonocarboxylate Transport I Inhibitor, SLC16A1 Inhibitor
References
ReferencesDoherty, J., et al. 2014. Cancer Res. 73,908.
Murray, C., et al. 2013. Nature. Chem. Biol. 1, 371.
Product Information
CAS number227321-12-2
FormWhite powder
Hill FormulaC₂₅H₂₉N₃O₂S
Chemical formulaC₂₅H₂₉N₃O₂S
Quality LevelMQ200
Applications
Biological Information
Primary TargetMCT1
Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
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
Global Trade Item Number
Catalog Number GTIN
5.09663.0001 04055977240993

Documentation

MCT1 Inhibitor, SR13800 - CAS 227321-12-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Doherty, J., et al. 2014. Cancer Res. 73,908.
Murray, C., et al. 2013. Nature. Chem. Biol. 1, 371.
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.

Revision28-April-2014 JSW
SynonymsMonocarboxylate Transport I Inhibitor, SLC16A1 Inhibitor
DescriptionA cell-permeable pyrole pyrimidine-based compound that acts as an inhibitor of monocarboxylate transporter 1 (MCT1, SLC16A1) and blocks the proliferation of Raji Burkitt lymphoma (Raji BL) cells expressing MCT1 (EC50 = 5 nM). Also shown to inhibit the growth of MCF-7 breast cancer cells. Effectively increases intracellular lactate levels while reducing lactate export and intracellular ATP levels in Raji cells. However, it does not affect basal oxygen consumption or the mitochondrial mass in these cells. Delays or even eliminates tumor growth in NOD/SCID mice injected with Raji lymphoma cells. Acts synergistically with metformin (Cat. No. 317240) to block monocarboxylate transport and tumor growth in humans and in murine models. Their combined effect also reduces cellular levels of glutathione with concomitant increase in hydrogen peroxide levels, which increases the death of Raji BL cells.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
CAS number227321-12-2
Chemical formulaC₂₅H₂₉N₃O₂S
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
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
ReferencesDoherty, J., et al. 2014. Cancer Res. 73,908.
Murray, C., et al. 2013. Nature. Chem. Biol. 1, 371.