PX-12

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

目錄號：S7947 Purity: 99.99%

PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide)是一種有效的 thioredoxin-1 (Trx-1) 抑制劑，作用于 Trx-1 上 Cys73 的不可逆硫代烷基化。Phase 2。

PX-12 Chemical Structure

CAS: 141400-58-0

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	810.81	現(xiàn)貨
10mg	794.43	現(xiàn)貨
50mg	3087.63	現(xiàn)貨
200mg	7182.63	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

PX-12相關(guān)產(chǎn)品

相關(guān)化合物庫	代謝化合物庫抗癌代謝化合物庫谷氨酰胺代謝化合物庫糖代謝化合物庫脂代謝化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息(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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide)是一種有效的 thioredoxin-1 (Trx-1) 抑制劑，作用于 Trx-1 上 Cys73 的不可逆硫代烷基化。Phase 2。

靶點(diǎn)

Trx-1 ^[1]

體外研究(In Vitro)
體外研究活性	在MCF-7和HT-29細(xì)胞中，PX-12防止低氧(1% 氧氣)誘導(dǎo)的HIF-1alpha蛋白增加，并降低HIF-1反式激活活性，VEGF形成，和誘導(dǎo)型一氧化氮合酶。PX-12也會抑制MCF-7和HT-29細(xì)胞的生長，IC50s分別為1.9 μM和2.9μM。^[1] PX-12也會通過Nrf2/PMF-1介導(dǎo)的增加抑制HIF-1α蛋白質(zhì)水平。^[2]在A549細(xì)胞中，PX-12通過G2/M細(xì)胞周期阻滯，和Bax-介導(dǎo)的，ROS-依賴性細(xì)胞凋亡抑制細(xì)胞生長。^[3]在肝癌細(xì)胞中，PX-12與5-FU發(fā)揮協(xié)同作用，顯著抑制致瘤性。^[4]
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	MCF-7 和 HT-29 細(xì)胞
	濃度	~10 μM
	孵育時(shí)間	72 小時(shí)
	方法	細(xì)胞生長使用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴鹽法測量。在空氣或低氧(1% 氧氣)條件下，細(xì)胞在一系列濃度的PX-12或pleurotin中暴露16小時(shí)。然后細(xì)胞在空氣中用溫的不含藥物的培養(yǎng)基洗滌，再進(jìn)行后面的72小時(shí)培育。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在負(fù)荷MCF-7腫瘤異種移植物的小鼠中，PX-12 (12 mg/kg, i.p.)降低HIF-1α 與 VEGF蛋白質(zhì)水平和微血管密度。^[1]
動(dòng)物實(shí)驗(yàn)	Animal Models	負(fù)荷MCF-7腫瘤異種移植物的小鼠
	Dosages	12 mg/kg
	Administration	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (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

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/12657718/ https://pubmed.ncbi.nlm.nih.gov/21069338/ https://pubmed.ncbi.nlm.nih.gov/24172913/ https://pubmed.ncbi.nlm.nih.gov/26550453/ + 展開

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/12657718/
https://pubmed.ncbi.nlm.nih.gov/21069338/
https://pubmed.ncbi.nlm.nih.gov/24172913/

https://pubmed.ncbi.nlm.nih.gov/26550453/

+ 展開

化學(xué)信息&溶解度

分子量	188.31	分子式	C₇H₁₂N₂S₂
CAS號	141400-58-0	SDF	Download PX-12 SDF
Smiles	CCC(C)SSC1=NC=CN1
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 38 mg/mL ( (201.79 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 38 mg/mL (201.79 mM)

Water : Insoluble

DMSO : 38 mg/mL ( (201.79 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 38 mg/mL (201.79 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動(dòng)物體內(nèi)配方計(jì)算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 Corn oil 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	2.400mg/ml (12.74mM)	以 1 mL 工作液為例，取50μL48mg/ml的澄清DMSO儲備液加到950μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 30%PEG300 2 65%ddH2O 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	1.200mg/ml (6.37mM)	以 1 mL 工作液為例,取50 μL 24mg/ml的澄清DMSO儲備液加到300 μL PEG300中,混合均勻使其澄清;向上述體系中加入650 μL ddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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