PX-12

別名：DB05448, 1-methyl propyl 2-imidazolyl disulfide

製品コード：S7947 純度：99.99%

PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.

CAS No. 141400-58-0

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫なし(納期7~10日)
10mg	JPY 22000	国内在庫なし(納期7~10日)
50mg	JPY 56500	国内在庫あり
200mg	JPY 131500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（11）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

PX-12関連製品

関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

Thioredoxin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
M21	Function assay	25 nM	16 hrs	Stimulation of nuclear translocation of thioredoxin-1 from cytosol in human M21 cells at 25 nM after 16 hrs by immunocytofluorescence	18617414
Raji	Function assay	5 to 10 uM	4 to 24 hrs	Induction of Trx mRNA expression in human Raji cells at 5 to 10 uM after 4 to 24 hrs by RT-PCR analysis	22128876
Raji	Function assay	10 to 20 uM	4 to 8 hrs	Induction of Trx protein expression in human Raji cells at 10 to 20 uM after 4 to 8 hrs by Western blot analysis	22128876
T84	Function assay		3 hrs	Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis, IC50=2.11μM	23327656
Ramos	Cytotoxicity assay		72 hrs	Cytotoxicity against human Ramos cells after 72 hrs by MTT assay, LD50=3.4μM	22128876
PancO2	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse PancO2 cells after 72 hrs by crystal violet staining, LD50=3.9μM	22128876
T24	Cytotoxicity assay		72 hrs	Cytotoxicity against human T24 cells after 72 hrs by crystal violet staining, LD50=4.6μM	22128876
B78	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse B78 cells after 72 hrs by crystal violet staining, LD50=5μM	22128876
CT26	Cytotoxicity assay		72 hrs	Cytotoxicity against wild type mouse CT26 cells after 72 hrs by crystal violet staining, LD50=5.2μM	22128876
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, LD50=5.5μM	22128876
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM	18617414
M21	Antiproliferative assay		48 hrs	Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM	18617414
Raji	Cytotoxicity assay		72 hrs	Cytotoxicity against human Raji cells after 72 hrs by MTT assay, LD50=8.8μM	22128876
EMT6	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse EMT6 cells after 72 hrs by crystal violet staining, LD50=11.6μM	22128876
HT29	Antiproliferative assay		48 hrs	Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method, GI50=25μM	18617414
MEF	Cytotoxicity assay			Cytotoxicity against mouse MEF cells, LD50=2.7μM	22128876
M21	Antiproliferative assay			Antiproliferative activity against human M21 cells, GI50=8.3μM	18502639
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells, GI50=8.3μM	18502639
HT29	Antiproliferative assay			Antiproliferative activity against human HT29 cells, GI50=25μM	18502639
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
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生物活性

製品説明

PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.

Targets

Trx-1 ^[1]

In Vitro
In vitro	In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9μM, respectively. ^[1] PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. ^[2] In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. ^[3] In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. ^[4]
細胞実験	細胞株	MCF-7 and HT-29 cells
	濃度	~10 μM
	反応時間	72 h
	実験の流れ	Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.

In Vivo
In Vivo	In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. ^[1]
動物実験	動物モデル	Mice bearing MCF-7 tumor xenografts
	投与量	12 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00736372	Completed	Metastatic Cancer\|Advanced Cancer	Cascadian Therapeutics Inc.\|Seagen Inc.	June 2008	Phase 1
NCT00417287	Terminated	Pancreatic Neoplasms	Cascadian Therapeutics Inc.\|National Cancer Institute (NCI)\|Translational Genomics Research Institute\|Seagen Inc.	December 2006	Phase 2

参考
[1] Welsh SJ, et al. Mol Cancer Ther. 2003, 2(3), 235-243. [2] Kim YH, et al. Cancer Chemother Pharmacol. 2011, 68(2), 405-413. [3] You BR, et al. Int J Oncol. 2014, 44(1), 301-308. [4] Li GZ, et al. Am J Transl Res. 2015, 7(9), 1528-1540. + 展開

参考

[4] Li GZ, et al. Am J Transl Res. 2015, 7(9), 1528-1540.

+ 展開

化学情報

分子量	188.31	化学式	C₇H₁₂N₂S₂
CAS No.	141400-58-0	SDF	Download PX-12 SDFをダウンロードする
Smiles	CCC(C)SSC1=NC=CN1
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 38 mg/mL ( (201.79 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 38 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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