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533871 Eph Receptor Antagonist, UniPR129 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₆H₅₂N₂O₄

Products

Catalog NumberPackaging Qty/Pack
5.33871.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable L-homo-Trp conjugate of lithocholic acid that acts as an Eph receptor antagonist and competitively disrupts Eph2A-ephrin-A1 binding (IC50 = 945 nM; KI = 345 nM). Blocks the interaction of ephrin-A1 and ephrin-B1 with all Eph receptors (IC50 = 840 nM - 1.54 µM for EphA and 2.6 - 3.74 µM for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µM), however, it does not affect tyrosine kinase activity of EGF and VEGF receptors. Slightly reduces PC3 cell proliferation without affecting cell cycle or apoptosis. However, it blocks the rounding effect of ephrin-A1-Fc in PC3 cells (IC50 = 6.25 µM). Also shown to inhibit angiogenesis in HUVEC (IC50 = 5.2 µM) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µM, respectively).

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 Number533871
Brand Family Calbiochem®
Synonyms(S)-3-((R)-4-((3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)-4-(1H-indol-3-yl)butanoic acid, Eph Inhibitor, UniPR129
References
ReferencesHassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm. 171, 5195.
Product Information
FormOff-white solid
Hill FormulaC₃₆H₅₂N₂O₄
Chemical formulaC₃₆H₅₂N₂O₄
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetEph Receptors
Primary Target IC<sub>50</sub>945 nM, Ki
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 -20°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
5.33871.0001 04055977286793

Documentation

Eph Receptor Antagonist, UniPR129 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Hassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm. 171, 5195.
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.

Revision30-January-2017 JSW
Synonyms(S)-3-((R)-4-((3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)-4-(1H-indol-3-yl)butanoic acid, Eph Inhibitor, UniPR129
DescriptionA cell-permeable L-homo-Trp conjugate of lithocholic acid that acts as an Eph receptor antagonist and competitively disrupts Eph2A-ephrin-A1 binding (IC50 = 945 nM; KI = 345 nM). Blocks the interaction of ephrin-A1 and ephrin-B1 with all Eph receptors (IC50 = 840 nM - 1.54 µM for EphA and 2.6 - 3.74 µM for EphB). Shown to inhibit EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µM), however, it does not affect tyrosine kinase activity of EGF and VEGF receptors. Slightly reduces PC3 cell proliferation without affecting cell cycle or apoptosis. However, it blocks the rounding effect of ephrin-A1-Fc in PC3 cells (IC50 = 6.25 µM). Also shown to inhibit angiogenesis in HUVEC (IC50 = 5.2 µM) and reduce ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µM, respectively).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₆H₅₂N₂O₄
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°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
ReferencesHassan-Mohamed, I., et al. 2014. Brit. Journ. Pharm. 171, 5195.