规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO |
|
||
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
体外研究 (In Vitro) |
Vadimezan (DMXAA) 是 I 型干扰素和其他细胞因子的强诱导剂、血管干扰剂和干扰素基因刺激剂 (STING) 的小鼠激动剂。 vadimezan (DMXAA) 对 344SQ-ELuc 细胞的活力没有负面影响。研究表明,M2 巨噬细胞中 p65 磷酸化增强表明 Vadimezan 介导的 NF-κB 通路激活 [1]。研究结果表明,与培养基预处理的巨噬细胞相比,Vadimezan (DMXAA) 处理的细胞在所有 MOI 下均能免受 VSV 诱导的细胞毒性。 vadimezan (DMXAA) 成功抑制了两种流感病毒株,表明该药物具有治疗人类流感耐药株的潜力[2]。
|
||
---|---|---|---|
体内研究 (In Vivo) |
Vadimezan (DMXAA) 注射后显着降低 344SQ-ELuc NSCLC 皮下肿瘤的生物发光 (BLI) 信号。当对 344SQ-ELuc 转移瘤施用 vadimezan (DMXAA) 时,光子发射率不会下降,并且肿瘤仍保持与对照的组织学相似性。当患有微小皮下肿瘤的小鼠接受 Vadimezan (DMXAA) 治疗时,光子输出在 6 小时和 24 小时内下降约 2 个对数单位,就像大型皮下肿瘤一样 [1]。当对感染流感的小鼠腹膜内给药时,Vadimezan (DMXAA) 是一种强度较低的 IFN-β mRNA 诱导剂,也是一种相当差的体内 TNF-α mRNA 诱导剂[2]。
|
||
动物实验 |
|
||
参考文献 |
[1]. Downey CM, et al. DMXAA causes tumor site-specific vascular disruption in murine non-small cell lung cancer, and like the endogenous non-canonical cyclic dinucleotide STING agonist, 2'3'-cGAMP, induces M2 macrophage repolarization. PLoS One. 2014 Jun 18;9
[2]. Shirey KA, et al. The anti-tumor agent, 5,6-dimethylxanthenone-4-acetic acid (DMXAA), induces IFN-beta-mediated antiviral activity in vitro and in vivo. J Leukoc Biol. 2011 Mar;89(3):351-7 |
分子式 |
C17H14O4
|
|
---|---|---|
分子量 |
282.29
|
|
CAS号 |
117570-53-3
|
|
相关CAS号 |
|
|
SMILES |
O=C(O)CC1=CC=CC(C2=O)=C1OC3=C2C=CC(C)=C3C
|
|
化学名 |
(5,6-Dimethyl-9-oxo-9H-xanthen-4-yl)-acetic acid
|
|
别名 |
NSC 640488, NSC-640488, NSC640488, ASA-404, Vadimezan; ASA404; ASA 404; AS1404; AS 1404; AS1404; DMXAA
|
|
存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
溶解度 (体外) |
|
|||
---|---|---|---|---|
溶解度 (体内) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (2.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 0.71 mg/mL (2.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL Solubility in Formulation 4: 5 mg/mL (17.71 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5425 mL | 17.7123 mL | 35.4246 mL | |
5 mM | 0.7085 mL | 3.5425 mL | 7.0849 mL | |
10 mM | 0.3542 mL | 1.7712 mL | 3.5425 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01299415 | Terminated | Drug: Vadimezan™ | Solid Tumors | Novartis Pharmaceuticals | August 2009 | Phase 1 |
NCT01285453 | Completed | Drug: vadimezan | Advanced or Recurrent Solid Tumors | Novartis Pharmaceuticals | March 2009 | Phase 1 |
NCT01290380 | Terminated | Drug: ASA404, DMXAA, DXAA | Solid Tumor Malignancies | Novartis Pharmaceuticals | February 2010 | Phase 1 |
NCT01299701 | Terminated | Drug: ASA404 | Advanced Solid Tumors | Novartis Pharmaceuticals | December 2008 | Phase 1 |
DMXAA inhibits influenza A/Wuhan and Tamiflu®-resistant influenza A/Br replication in vitro.J Leukoc Biol.2011 Mar;89(3):351-7. td> |
Differential induction of IFN-β and TNF-α mRNA expression by DMXAA and LPS in vivo.J Leukoc Biol.2011 Mar;89(3):351-7. td> |
IFN-β-dependent, DMXAA-mediated protection of mice against influenza-induced lethality.J Leukoc Biol.2011 Mar;89(3):351-7. td> |