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

521275
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₀H₄N₆O 331253-86-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      521275-5MG
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          Glass bottle 5 mg
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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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          Biologics 33.1 ( 1.37 MB )
          Biologics 33.2
          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 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.