521275 PDK1/Akt/Flt Dual Pathway Inhibitor - CAS 331253-86-2 - Calbiochem

521275
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₁₀H₄N₆O 331253-86-2

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521275-5MG
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      Description
      OverviewA cell-permeable compound that selectively induces apoptosis in AML (Acute Myelogenous Leukemia) with little effect on normal CD34+ AML progenitor cells. Shown to directly inhibit both PDK1 and Akt activities in in vitro kinase assays in a dose-dependent manner and block cellular phosphorylation of Akt at both Ser473 and Thr308. The dual inhibition nature against both PDK1/Akt and Flt3/PIM signaling pathways allows effective killing of AML cells (Average IC50 = 1.05, 1.91, and 0.43 µM for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively) that are otherwise resistant to inhibitors that target only the PDK1/Akt pathway.
      CAS. Nos. 331253-86-2 and 329710-24-9 (two isomers)
      Catalogue Number521275
      Brand Family Calbiochem®
      Synonyms6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one & 10H-Indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one, Akt Inhibitor XXI, PDK1 Inhibitor I, KP372-1
      References
      ReferencesZeng, Z., et al. 2006. Cancer Res. 66, 3737.
      Koul, D., et al. 2006. Mol. Cancer Ther. 5, 637.
      Mandal. M., et al. 2006. Oral Oncol. 42, 430.
      Mandal. M., et al. 2005. Br. J. Cancer 92, 1899.
      Product Information
      CAS number331253-86-2
      ATP CompetitiveN
      FormYellow solid
      Hill FormulaC₁₀H₄N₆O
      Chemical formulaC₁₀H₄N₆O
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetBoth PDK1 and Akt activities
      Primary Target IC<sub>50</sub>1.05, 1.91, and 0.43 µM for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively
      Purity≥98% by HPLC (sum of two isomers)
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 36/37/38

      Irritating to eyes, respiratory system and skin.
      S PhraseS: 26-36

      In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
      Wear suitable protective clothing.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Irritant
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PDK1/Akt/Flt Dual Pathway Inhibitor - CAS 331253-86-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PDK1/Akt/Flt Dual Pathway Inhibitor - CAS 331253-86-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      521275

      References

      Reference overview
      Zeng, Z., et al. 2006. Cancer Res. 66, 3737.
      Koul, D., et al. 2006. Mol. Cancer Ther. 5, 637.
      Mandal. M., et al. 2006. Oral Oncol. 42, 430.
      Mandal. M., et al. 2005. Br. J. Cancer 92, 1899.
      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.

      Revision18-April-2011 RFH
      Synonyms6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one & 10H-Indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one, Akt Inhibitor XXI, PDK1 Inhibitor I, KP372-1
      DescriptionA cell-permeable compound that selectively induces apoptosis in AML (Acute Myelogenous Leukemia) with little effect on normal CD34+ AML progenitor cells. Shown to directly inhibit both PDK1 and Akt activities in in vitro kinase assays in a dose-dependent manner and block cellular phosphorylation of Akt at both Ser473 and Thr308. The dual inhibition nature against both PDK1/Akt and Flt3/PIM signaling pathways allows effective killing of AML cells (Average IC50 = 1.05, 1.91, and 0.43 µM for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively) that are otherwise resistant to inhibitors that target only the PDK1/Akt pathway. CAS. No. 331253-86-2 and 329710-24-9.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number331253-86-2
      Chemical formulaC₁₀H₄N₆O
      Structure formulaStructure formula
      Purity≥98% by HPLC (sum of two isomers)
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Irritant
      ReferencesZeng, Z., et al. 2006. Cancer Res. 66, 3737.
      Koul, D., et al. 2006. Mol. Cancer Ther. 5, 637.
      Mandal. M., et al. 2006. Oral Oncol. 42, 430.
      Mandal. M., et al. 2005. Br. J. Cancer 92, 1899.