数量	カタログ番号	注文内容	Qty/Pk	価格
			96-Well Plate

数量	カタログ番号	注文内容	Qty/Pk	価格
	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

509880 Sigma-AldrichIDH2 Inhibitor, R140Q Somatic Mutant-Specific, AGI-6780 - CAS 1432660-47-3 - Calbiochem

A cell-permeable inhibitor of isocitrate dehydrogenase 2 R140Q mutant-containing dimers. Has minimal effect on wild type dimer-catalyzed alpha-KG production.

IDH2 Inhibitor, R140Q Somatic Mutant-Specific, AGI-6780 - CAS 1432660-47-3 - Calbiochem: のSDS（安全データシート）、CoA（試験成績書）およびCoQ（品質証明書）、カタログなど製品関連の技術資料を入手いただけます。

(M)SDS
参考資料
Data Sheet

同義語: Isocitrate Dehydrogenase 2 R140 Somatic Mutant Inhibitor, AGI6780

Primary Target: (IDH2) R140Q mutants

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概要

Replacement Information

主要スペック表

CAS #	Empirical Formula
1432660-47-3	C₂₁H₁₈F₃N₃O₃S₂

価格＆在庫状況

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Description
Overview	A cell-permeable urea sulfonamide that inhibits the activity of Isocitrate Dehydrogenase 2 (IDH2) R140Q mutant-containing dimers in an α-ketoglutarate/α-KG-non-competitive and NADPH-uncompetitive manner by stabilizing the mutant dimers in an inactive conformation via a high-affinity allosteric interaction at the dimer interface with a slow-binding kinetic (k_on = 5.8 x 10⁴/M/min; k_off = 8.3 x 10^-3/min), while displaying much reduced potency against wt IDH2 dimer-catalyzed α-KG production and little or no activity toward wt IDH1 or R132H IDH2 mutant. Selectively inhibits 2-HG production in IDH2 R140Q, but not R132H, mutant-expressing U87 cultures (IC₅₀ in 48 h = 11 nM vs. >100 µM). AGI-6780 treatment (5 µM) of primary bone marrow cultures from AML patients with R140Q mutation is shown to reactivate the differentiation of immature AML blasts without cytotoxicity.
Catalogue Number	509880
Brand Family	Calbiochem®
Synonyms	Isocitrate Dehydrogenase 2 R140 Somatic Mutant Inhibitor, AGI6780

References
References	Wang, F., et al. 2013. Science 340, 622.

Product Information
CAS number	1432660-47-3
Form	Off-white powder
Hill Formula	C₂₁H₁₈F₃N₃O₃S₂
Chemical formula	C₂₁H₁₈F₃N₃O₃S₂
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	(IDH2) R140Q mutants
Primary Target IC<sub>50</sub>	4 nM/16 h & 120 nM/1 h against R140Q-wt heterodimer
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
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
カタログ番号	GTIN
5.09880.0001	04055977241112

Documentation

IDH2 Inhibitor, R140Q Somatic Mutant-Specific, AGI-6780 - CAS 1432660-47-3 - Calbiochem (M)SDS

タイトル
英語版製品安全データシート（(M)SDS）

参考資料

参考資料の概要
Wang, F., et al. 2013. Science 340, 622.

データシート

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	29-April-2014 JSW
Synonyms	Isocitrate Dehydrogenase 2 R140 Somatic Mutant Inhibitor, AGI6780
Description	A cell-permeable ureido-benzenesulfonamide that inhibits α-ketoglutarate (α-KG)-to-(R)-2-hydroxyglutarate (2-HG) conversion catalyzed by Isocitrate Dehydrogenase-2 (IDH2) R140Q mutant-containing dimers (IC₅₀/preincubation time = 4 nM/16 h & 120 nM/1 h against R140Q-wt heterodimer; 23 nM/16 h & 170 nM/1 h against R140Q homodimer) in a substrate-non-competitive and NADPH-uncompetitive manner by targeting the dimer interface via a high affinity allosteric interaction with a slow-binding kinetic (k_on = 5.8 x 10⁴/M/min; k_off = 8.3 x 10^-3/min) and stabilizing the mutant dimers in an inactive conformation, while displaying much reduced potency against wt IDH2 dimer-catalyzed α-KG production (IC₅₀/preincubation time = 190 nM/16 h & 2.7 µM/1 h) and little or no activity toward LDHA, 3PGDH, GDH, G6PDH, R132H mutant or wt IDH1. Selectively inhibits 2-HG production in R140Q IDH2-expressing U87 glioblastoma & TF-1 erythroleukemia, but not R132H-expressing U87 cultures (IC₅₀ in 48 h = 11 nM, 18 nM, and >100 µM, respectively) and sensitizes R140Q IDH2-expressing TF-1 to EPO-induced erythroid differentiation. Likewise, inhibition of 2-HG production in primary bone marrow cultures from AML patients with R140Q mutation (complete inhibition with 5 µM AGI-6780) is shown to reactivate the differentiation of immature AML blasts without cytotoxicity. IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 (Cat. No. 410972) is also available.
Form	Off-white powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1432660-47-3
Chemical formula	C₂₁H₁₈F₃N₃O₃S₂
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (100 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	Standard Handling
References	Wang, F., et al. 2013. Science 340, 622.

カテゴリー

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest

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