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

The PDK1/Akt/Flt Dual Pathway Inhibitor, also referenced under CAS 331253-86-2, controls the biological activity of PDK1/Akt/Flt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: Both PDK1 and Akt activities
521275
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
331253-86-2C₁₀H₄N₆O

Products

Catalogue NumberPackaging Qty/Pack
521275-5MG Plastic ampoule 5 mg
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
Global Trade Item Number
Catalogue Number GTIN
521275-5MG 04055977271447

Documentation

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.

Brochure

Title
Akt

Posters

Title
Human Kinome & InhibitorSelect™ Libraries
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 Protect from light
+2°C to +8°C
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.