PX-12

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

目錄號(hào)：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
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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

PX-12相關(guān)產(chǎn)品

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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
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(huì)抑制MCF-7和HT-29細(xì)胞的生長(zhǎng)，IC50s分別為1.9 μM和2.9μM。^[1] PX-12也會(huì)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(zhǎng)。^[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(zhǎng)使用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴鹽法測(cè)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)
[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

參考文獻(xiàn)

[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

化學(xué)信息&溶解度

分子量	188.31	分子式	C₇H₁₂N₂S₂
CAS號(hào)	141400-58-0	SDF	Download PX-12 SDF
Smiles	CCC(C)SSC1=NC=CN1
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)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(huì)降低化合物溶解度，請(qǐng)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(huì)降低化合物溶解度，請(qǐng)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)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)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

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(qǐng)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(qǐng)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(qǐng)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(qǐng)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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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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