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			96-Well Plate

数量	产品目录编号	订购说明	数量 / 包装	公开价
	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

521275 Sigma-AldrichPDK1/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.

分析证书
参考
小册子
Data Sheet
Posters

同义词: 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

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
331253-86-2	C₁₀H₄N₆O

价格及供货情况

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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.
Overview	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
Reversible	N
Structure formula Image
Quality Level	MQ100

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

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	Ok to freeze
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

Global Trade Item Number
产品目录编号	GTIN
521275-5MGCN	04055977271447

Documentation

PDK1/Akt/Flt Dual Pathway Inhibitor - CAS 331253-86-2 - Calbiochem 分析证书

标题	批号
521275	输入批号

参考

参考信息概述
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.

小册子

标题
Akt

海报

标题
Human Kinome & InhibitorSelect™ Libraries

数据表

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
Chemical formula	C₁₀H₄N₆O
Structure formula
Purity	≥98% by HPLC (sum of two isomers)
Solubility	DMSO (10 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Akt (Protein Kinase B) Inhibitors

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