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Vadimezan (DMXAA)

別名: ASA404, NSC 640488 中文名稱：2,5-己酮可可堿

Vadimezan (DMXAA)是一種vascular disrupting agents (VDA)，也是一種DT-diaphorase的競(jìng)爭(zhēng)性抑制劑，無(wú)細(xì)胞試驗(yàn)中Ki為20 μM ，IC50為62.5 μM。DMXAA (Vadimezan) 也是一種STING 激動(dòng)劑，具有潛在的抗腫瘤活性。DMXAA (Vadimezan) 在體外可有效誘導(dǎo) IFN-β 和 TNF-α 的表達(dá)，但對(duì) TNF-α 影響相對(duì)較低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。

Vadimezan (DMXAA) Chemical Structure

Vadimezan (DMXAA) Chemical Structure

CAS: 117570-53-3

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1138.26 現(xiàn)貨
5mg 991.09 現(xiàn)貨
10mg 1613.58 現(xiàn)貨
25mg 3029.34 現(xiàn)貨
100mg 7922.67 現(xiàn)貨
1g 12039.3 現(xiàn)貨
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Vadimezan (DMXAA)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

VDA Signaling Pathways

VDA信號(hào)通路圖

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
MDA-MB-231 Apoptosis assay 24 to 96 uM 48 hrs Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-3 expression at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Apoptosis assay 24 to 96 uM 48 hrs Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved PARP level at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Decrease in caspase-3 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Increase in p53 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Decrease in caspase-9 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
MDA-MB-231 Function assay 24 to 96 uM 48 hrs Decrease in MDM2 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis 28376372
HepG2 Cell cycle arrest assay 0.2 uM 24 hrs Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase at 0.2 uM after 24 hrs by propidium iodide staining-based flow cytometric method relative to control 29129511
HepG2 Apoptosis assay 0.2 uM 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 levels at 0.2 uM after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 0.2 uM 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-9 levels at 0.2 uM after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 0.2 uM 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP levels at 0.2 uM after 24 hrs by Western blot method 29129511
HECPP cells Function assay 10 ug/mL Activation of NF-kappaB in HECPP cells at 10 ug/mL 17616114
human BJ cells Cytotoxic?assay 24 h Cytotoxicity against human BJ cells after 24 hrs by MTT assay, CC50=48.9 μM 24518295
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 11.89 μM. 29129511
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 12.12 μM. 29129511
K562 Antiproliferative assay 24 hrs Antiproliferative activity against human K562 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 19.14 μM. 29129511
HepG2 Antiproliferative assay 24 hrs Antiproliferative activity against human HepG2 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 21.25 μM. 29129511
COLO320 Antiproliferative assay 48 hrs Antiproliferative activity against human COLO320 cells after 48 hrs by CCK8 assay, IC50 = 39.5 μM. 28376372
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50 = 48.4 μM. 28376372
MDA-MB-231 Growth inhibition assay 24 hrs Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 48.42 μM. 29609121
MDA-MB-231 Antiproliferative assay 24 hrs Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 48.44 μM. 29129511
HepG2 Cell cycle arrest assay 24 hrs Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by propidium iodide staining-based flow cytometric method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-9 levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as downregulation of Bcl-xL expression co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
HepG2 Apoptosis assay 24 hrs Induction of apoptosis in human HepG2 cells assessed as upregulation of Bid expression co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method 29129511
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH 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: Primary screen for NB1643 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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
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生物活性

產(chǎn)品描述 Vadimezan (DMXAA)是一種vascular disrupting agents (VDA)，也是一種DT-diaphorase的競(jìng)爭(zhēng)性抑制劑，無(wú)細(xì)胞試驗(yàn)中Ki為20 μM ，IC50為62.5 μM。DMXAA (Vadimezan) 也是一種STING 激動(dòng)劑，具有潛在的抗腫瘤活性。DMXAA (Vadimezan) 在體外可有效誘導(dǎo) IFN-β 和 TNF-α 的表達(dá)，但對(duì) TNF-α 影響相對(duì)較低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。
特性 DMXAA（ASA404)是DT-心肌黃酶競(jìng)爭(zhēng)性抑制劑。
靶點(diǎn)
DT-diaphorase [1]
(Cell-free assay)		 DT-diaphorase [1]
(Cell-free assay)
20 μM(Ki) 20 μM(Ki)
體外研究(In Vitro)
體外研究活性 在體外, DMXAA（ASA404)抑制純化的DT-心肌黃酶，IC50為62.5 μM，Ki為20 μM。DMXAA（ASA404)作用于DLD-1人結(jié)腸癌細(xì)胞, 抑制DT-心肌黃酶活性，IC50為 49.6 μM，而對(duì)細(xì)胞色素 b5 還原酶和細(xì)胞色素P450還原酶沒(méi)有顯著作用效果。[1] DMXAA（ASA404)為抗病毒藥物，作用于RAW 264.7巨噬細(xì)胞，抑制VSV-誘導(dǎo)的細(xì)胞毒性，也抑制流感病毒復(fù)制。[2] 最新研究顯示DMXAA（ASA404)作用于VEGFR幾種激酶成員,如人人臍靜脈內(nèi)皮細(xì)胞中的VEGFR2信號(hào)，具有非免疫調(diào)節(jié)的抑制效果。[3]
激酶實(shí)驗(yàn) DT-心肌黃酶活性和酶抑制動(dòng)力學(xué)分析
通過(guò)在Beckman DU 650分光光度計(jì)上檢測(cè)細(xì)胞色素 c 在 550 nm處減少量而測(cè)定純化的DT-心肌黃酶活性。每組實(shí)驗(yàn)含細(xì)胞色素c(70 μM), NADH(多種濃度), 純化的DT-心肌黃酶(0.032 μg),及溶于含0.14% BSA終體積為1 mL Tris–HCl buffer(50 mM, pH 7.4)的維生素K(多種濃度)。加入NADH開(kāi)始反應(yīng)。根據(jù)反應(yīng)曲線初始部分(30秒)計(jì)算減少率, 結(jié)果表示為μmol 減少的細(xì)胞色素/min/mg 蛋白，使用21 mM?1 cm?1 摩爾消光系數(shù)表示減少的細(xì)胞色素c。在室溫下進(jìn)行酶反應(yīng)，所有反應(yīng)做三次平行。反應(yīng)中含有的DMXAA（ASA404) (不同濃度) 用來(lái)表示純化的 DT-心肌黃酶抑制活性,通過(guò)改變NADH (維生素K不變)維生素K (NADH不變) 的濃度測(cè)定抑制特性。獲得Ki值。通過(guò)測(cè)量對(duì)Dicumarol敏感的DCPIP在 600 nm處的減少量而測(cè)定DT-心肌黃酶作用于DLD-1細(xì)胞的活性收集處于指數(shù)生長(zhǎng)中期的DLD-1細(xì)胞，置于冰凍buffer (Tris–HCl, 25 mM, pH 7.4和 250 mM蔗糖)，然后在冰上進(jìn)行超聲處理。酶反應(yīng)條件為2 mM NADH, 40 μM DCPIP, 溶于含BSA (0.7 mg/mL)終體積為1 mL Tris–HCl (25 mM, pH 7.4) 的 20 μL Dicumarol。使用21 mM?1 cm?1 的摩爾消光系數(shù)表示對(duì)Dicumarol敏感的 DCPIP減少量。通過(guò) Bradford檢測(cè)測(cè)定蛋白水平。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 DLD-1和 H460
濃度 0 到2 mM
孵育時(shí)間 96 小時(shí)
方法 DLD-1人結(jié)腸癌和H460人非小細(xì)胞肺癌細(xì)胞單層培養(yǎng)在RPMI 1640培養(yǎng)基中，培養(yǎng)基中補(bǔ)充胎牛血清 (10%), 丙酮酸鈉(2 mM), 青霉素/鏈霉親和素 (50 IU mL?1/50 μg mL-1) 及l(fā)-谷氨酰胺(2 mM)。在有氧條件下進(jìn)行MTT 實(shí)驗(yàn)和所有其他實(shí)驗(yàn)，檢測(cè)藥物敏感性。細(xì)胞接種在96孔板上，然后在含5% CO2的環(huán)境下溫育過(guò)夜。完全移除培養(yǎng)基，使用含多種藥物濃度的培養(yǎng)基替代。在只有維生素K時(shí)，藥物處理時(shí)間為1小時(shí),然后細(xì)胞在Hanks’平衡鹽溶液中沖洗兩次，然后在每孔中加入200 μL 新鮮RPMI 1640培養(yǎng)基。 在只有DMXAA（ASA404) 存在時(shí)，藥物處理時(shí)間為3小時(shí)。 隨后溫育4天，使用MTT檢測(cè)測(cè)定細(xì)胞存活情況。為了DMXAA（ASA404)和維生素K聯(lián)用，初步建立細(xì)胞 ，選擇非毒性(細(xì)胞存活率>95%)濃度的DMXAA（ASA404)。細(xì)胞使用DMXAA（ASA404) (2 mM)先處理2小時(shí)，隨后移除培養(yǎng)基，使用含抑制劑 (DMXAA（ASA404)，持續(xù)濃度為2 mM)和維生素K(多種濃度)的培養(yǎng)基更換。再溫育7小時(shí)，使用Hanks’平衡鹽溶液沖洗細(xì)胞，再加入生長(zhǎng)培養(yǎng)基。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-p38 / p38 p-MK2 / pERK / p-JNK 21819972
Growth inhibition assay Cell proliferation 30138430
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 DMXAA（ASA404)顯著延遲化學(xué)致癌物誘導(dǎo)的細(xì)胞生長(zhǎng), 提高腫瘤倍增時(shí)間，且提高從治療到安樂(lè)死的時(shí)間。DMXAA（ASA404)處理攜帶腫瘤的動(dòng)物后, 平均腫瘤倍增時(shí)間,平均腫瘤變?nèi)稌r(shí)間，及從治療到安樂(lè)死的平均時(shí)間分別提高4.4-, 1.8- 2.7-倍。[4] DMXAA（ASA404)處理顯著保護(hù)感染200 p.f.u.小鼠適應(yīng)的H1N1流感 PR8病毒的C57BL/6J小鼠，使存活率達(dá)60%, 而對(duì)照組存活率只為20%。[2]
動(dòng)物實(shí)驗(yàn) Animal Models 注射化學(xué)致癌物 (NMU)的雌性 Wistar大鼠
Dosages ≤300 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00856336 Completed
Refractory Tumors
Antisoma Research
 May 2003 Phase 1
NCT00863733 Completed
Solid Tumors
Cancer Research UK|Cancer Society Auckland
 May 1996 Phase 1

化學(xué)信息&溶解度

分子量 282.29 分子式

C17H14O4
CAS號(hào) 117570-53-3 SDF Download Vadimezan (DMXAA) SDF
Smiles CC1=C(C2=C(C=C1)C(=O)C3=CC=CC(=C3O2)CC(=O)O)C
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

7.5%Sodium bicarbonate : 10 mg/mL (35.42 mM)

DMSO : 7 mg/mL ( (24.79 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

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

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(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 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(guò)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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