Vadimezan (DMXAA)

別名: ASA404, NSC 640488 中文名稱：2,5-己酮可可堿

目錄號：S1537 Purity: 99.94%

Vadimezan (DMXAA)是一種vascular disrupting agents (VDA)，也是一種DT-diaphorase的競爭性抑制劑，無細(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 TNF-α 影響相對較低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。

Vadimezan (DMXAA) Chemical Structure

CAS: 117570-53-3

規(guī)格	價(jià)格	庫存
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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產(chǎn)品質(zhì)控

批次：純度： 99.94%

99.94

Vadimezan (DMXAA)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
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

DMXAA（ASA404)是DT-心肌黃酶競爭性抑制劑。

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，K_i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，而對細(xì)胞色素 b5 還原酶和細(xì)胞色素P450還原酶沒有顯著作用效果。^[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，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力學(xué)分析
激酶實(shí)驗(yàn)	通過在Beckman DU 650分光光度計(jì)上檢測細(xì)胞色素 c 在 550 nm處減少量而測定純化的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) 用來表示純化的 DT-心肌黃酶抑制活性,通過改變NADH (維生素K不變)維生素K (NADH不變) 的濃度測定抑制特性。獲得K_i值。通過測量對Dicumarol敏感的DCPIP在 600 nm處的減少量而測定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Dicumarol敏感的 DCPIP減少量。通過 Bradford檢測測定蛋白水平。
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檢測測定細(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，再加入生長培養(yǎng)基。
實(shí)驗(yàn)圖片	檢測方法	檢測指標(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, 提高腫瘤倍增時(shí)間，且提高從治療到安樂死的時(shí)間。DMXAA（ASA404)處理攜帶腫瘤的動物后, 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%, 而對照組存活率只為20%。^[2]
動物實(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
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00856336	Completed	Refractory Tumors	Antisoma Research	May 2003	Phase 1
NCT00863733	Completed	Solid Tumors	Cancer Research UK\|Cancer Society Auckland	May 1996	Phase 1

參考文獻(xiàn)
[1] Phillips RM. Biochem Pharmacol. 1999, 58(2), 303-310. [2] Shirey KA, et al. J Leukoc Biol. 2011, 89(3), 351-357. [3] Buchanan CM, et al. Clin Sci (Lond). 2012, 122(10), 449-457. [4] Liu JJ, et al. Cancer Chemother Pharmacol. 2007, 59(5), 661-669. + 展開

參考文獻(xiàn)

[1] Phillips RM. Biochem Pharmacol. 1999, 58(2), 303-310.
[2] Shirey KA, et al. J Leukoc Biol. 2011, 89(3), 351-357.
[3] Buchanan CM, et al. Clin Sci (Lond). 2012, 122(10), 449-457.

[4] Liu JJ, et al. Cancer Chemother Pharmacol. 2007, 59(5), 661-669.

+ 展開

化學(xué)信息&溶解度

分子量	282.29	分子式	C₁₇H₁₄O₄
CAS號	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：

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

DMSO : 7 mg/mL ( (24.79 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

DMSO : 4 mg/mL ( (14.16 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 10.9 mg/mL ( (38.61 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 13 mg/mL ( (46.05 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 6 mg/mL ( (21.25 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度批次：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					動物體內(nèi)配方計(jì)算器
體內(nèi)溶解度批次：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	澄清溶液	7.5% sodium bicarbonate	10.0mg/ml (35.42mM)	取10mg 產(chǎn)品溶解于1ml 7.5% Sodium bicarbonate（7.5%碳酸氫鈉溶液）中，超聲加熱五分鐘至澄清溶液。	動物體內(nèi)配方計(jì)算器
澄清溶液	8% DMSO 1 40% PEG 300 2 5%Tween80 3 47% water	0.24mg/ml (0.85mM)	以 1 mL 工作液為例,取80 μL 3mg/ml的澄清DMSO儲備液加到400 μL PEG300中,混合均勻使其澄清;向上述體系中加入50 μL Tween80,混合均勻使其澄清;然后繼續(xù)加入470 μL ddH2O定容至1 mL。工作液請現(xiàn)配現(xiàn)用!
澄清溶液	10% DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	0.75mg/ml (2.66mM)	以 1 mL 工作液為例,取100 μL 7.5mg/ml的澄清DMSO儲備液加到400 μL PEG300中,混合均勻使其澄清;向上述體系中加入50 μL Tween80,混合均勻使其澄清;然后繼續(xù)加入450 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，建議多配一只動物的藥量）

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

第二步：請輸入動物體內(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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* 必填項(xiàng)

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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