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121762 AG 957, Adamantyl Ester

121762
  
Purchase on Sigma-Aldrich

Overview

Replacement Information
Description
Overview

This product has been discontinued.

Please refer to our complete listing of Protein Tyrosine Kinase Inhibitors for a possible alternative. Please read the alternative product documentation carefully and contact technical service if you need additional information.





A lipophilic, adamantyl ester form of tyrphostin AG 957 (Cat. No. 121761) that displays antiproliferative properties. Shown to be selective and ~3-4 fold more potent than the bcr/abl kinase inhibitor AG 957. Has a longer serum half-life in vivo. Downregulates p210bcr/abl autokinase activity (IC50 = 14 µM). Selectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC50 = 9.8 µM) by inducing apoptosis. Reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC50 ~0.1-0.25 µM).
Catalogue Number121762
Brand Family Calbiochem®
Synonyms4-Amino-N-(2,5-dihydroxybenzyl)adamantyl Benzoate, 4-(2,5-Dihydroxy-benzylamino)benzoic Acid Adamantan-1-yl Ester
References
ReferencesAvramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479.
Mow, B.M., et al. 2002. Blood 99, 664.
Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.
Product Information
FormOff-white solid
Hill FormulaC₂₄H₂₇NO₄
Chemical formulaC₂₄H₂₇NO₄
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary Targetp210bcr-abl
Primary Target IC<sub>50</sub>14 µM
Secondary targetSelectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC₅₀ = 9.8 µM)
Purity≥ 97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Blue Ice Only
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). DMSO stock solutions are stable for up to 3 weeks at -20°C. Ethanol 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

Documentation

AG 957, Adamantyl Ester Certificates of Analysis

TitleLot Number
121762

References

Reference overview
Avramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479.
Mow, B.M., et al. 2002. Blood 99, 664.
Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.
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.

Revision02-June-2010 JSW
Synonyms4-Amino-N-(2,5-dihydroxybenzyl)adamantyl Benzoate, 4-(2,5-Dihydroxy-benzylamino)benzoic Acid Adamantan-1-yl Ester
DescriptionA lipophilic, adamantyl ester form of tyrphostin AG 957 (Cat. No. 121761) that displays anti-proliferative properties. Shown to be selective and ~3-4 fold more potent than AG 957 as a bcr/abl kinase inhibitor. Also exhibits a longer serum half-life in vivo. Down-regulates p210bcr/abl autokinase activity (IC50 = 14 µM), selectively blocks granulocyte colony formation in chronic myelogenous leukemia (CML) progenitors (median IC50 = 12 µM), and inhibits proliferation of K562 cells (IC50 = 9.8 µM) by inducing apoptosis. Also blocks protein synthesis and VEGF secretion. Reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC50 ~100-250 nM).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₄H₂₇NO₄
Structure formulaStructure formula
Purity≥ 97% by HPLC
SolubilityDMSO (10 mg/ml) or Ethanol (5 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 3 weeks at -20°C. Ethanol stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesAvramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479.
Mow, B.M., et al. 2002. Blood 99, 664.
Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.