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400036 Glucose Transporter Inhibitor IV, WZB117 - CAS 1223397-11-2 - Calbiochem

400036
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Replacement Information

Tabella delle specifiche principali

CAS #Empirical Formula
1223397-11-2C₂₀H₁₃FO₆

Products

Numero di catalogoConfezionamento Qtà/conf
400036-25MG Bottiglia di vetro 25 mg
Description
OverviewA bis-hydroxybenzoate compound that acts as a fast-acting, irreversible blocker of glucose transport by GLUT1 in red blood cells. Shown to rapidly inhibit glucose transport in cancer cells (IC50 ~ 500 nM in A549 cells) and block proliferation. Its inhibitory effects are more pronounced in hypoxic cancer cells. It binds directly to GLUT1 involving three hydrogen bonds, one each with Asn34, Arg126, and Trp412. Also shown to reduce the levels of GLUT1 protein, intracellular ATP levels, and glycolytic enzymes and increase the level of AMPK in tumor cells. Preferentially induces cell cycle arrest and causes senescence and necrosis in red blood cells and tumor cells (IC50 = 10 µM) over non cancerous cells and synergizes the anti-tumor effects of cisplatin (Cat. No. 232120) and paclitaxel (Cat. No. 580555). Also, effectively suppresses tumor growth in human A549 lung cancer grafted nude mice model (10 mg/kg, i.p., daily).
Catalogue Number400036
Brand Family Calbiochem®
SynonymsGLUT Inhibitor IV, WZB117, 3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate)
References
ReferencesLiu. Y., et al. 2012. Mol. Cancer Ther. 11, 1672.
Product Information
CAS number1223397-11-2
FormWhite powder
Hill FormulaC₂₀H₁₃FO₆
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationGlucose Transporter Inhibitor IV, WZB117, CAS 1223397-11-2, is a fast-acting, irreversible blocker of GLUT1 in RBCs. Also inhibits glucose transport in cancer cells (IC50 ~ 500 nM in A549 cells).
Biological Information
Primary TargetGlut1
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 Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Protect from Moisture Protect from moisture
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C. Unstable in DMSO.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Panoramica delle referenze
Liu. Y., et al. 2012. Mol. Cancer Ther. 11, 1672.
Scheda tecnica

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.

Revision27-September-2013 JSW
SynonymsGLUT Inhibitor IV, WZB117, 3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate)
DescriptionA bis-hydroxybenzoate compound that acts as a fast-acting, irreversible blocker of glucose transport by GLUT1 in red blood cells. Shown to rapidly inhibit glucose transport in cancer cells (IC50 ~ 500 nM in A549 cells) and block proliferation. Its inhibitory effects are more pronounced in hypoxic cancer cells. It binds directly to GLUT1 involving three hydrogen bonds, one each with Asn34, Arg126, and Trp412. Also shown to reduce the levels of GLUT1 protein, intracellular ATP levels, and glycolytic enzymes and increase the level of AMPK in tumor cells. Preferentially induces cell cycle arrest and causes senescence and necrosis in red blood cells and tumor cells (IC50 = 10 µM) over non cancerous cells and synergizes the anti-tumor effects of cisplatin (Cat. No. 232120) and paclitaxel (Cat. No. 580555). Also, effectively suppresses tumor growth in human A549 lung cancer grafted nude mice model (10 mg/kg, i.p., daily).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1223397-11-2
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityEthanol (100 mg/ml)
Storage -20°C
Protect from moisture
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C. Unstable in DMSO.
Toxicity Standard Handling
ReferencesLiu. Y., et al. 2012. Mol. Cancer Ther. 11, 1672.