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

521275
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      Overview

      Key Spec Table

      Empirical FormulaCAS #
      C₁₀H₄N₆O331253-86-2

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      521275-5MG
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      Discontinued
      There is a newer version of this product
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          5 mg
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          Description
          Overview A 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 Number 521275
          Brand Family Calbiochem®
          Synonyms 6H-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
          References 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.
          Product Information
          CAS number 331253-86-2
          ATP Competitive N
          Form Yellow solid
          Hill Formula C₁₀H₄N₆O
          Chemical formula C₁₀H₄N₆O
          Molar Mass 224.2
          Reversible N
          Structure formula Image
          Applications
          Biological Information
          Primary Target Both 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 permeable Y
          Solubility DMSO
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          R Phrase R: 36/37/38

          Irritating to eyes, respiratory system and skin.
          S Phrase S: 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 No
          Special Instructions Following 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

          MSDS

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          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.

          Revision 18-April-2011 RFH
          Synonyms 6H-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
          Description A 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.
          Form Yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number 331253-86-2
          Molar mass 224.2
          Chemical formula C₁₀H₄N₆O
          Structure formula
          Purity ≥98% by HPLC (sum of two isomers)
          Solubility DMSO (10 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Irritant
          References 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.