规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mg |
|
||
5mg |
|
||
Other Sizes |
|
体外研究 (In Vitro) |
3,6-DMAD 盐酸盐对 MM 细胞系具有细胞毒性(0–6 μM;24 小时;RPMI 8226 和 MM1.R 人 MM 细胞)[1]。在用 Tg (0.3 μM) 处理 14 小时的 HT1080 细胞中,3,6-DMAD 盐酸盐 (0-30 μM) 以剂量依赖性方式抑制 XBP1 剪接 (XBP1s)[1]。 IRE1α核酸内切酶活性被3,6-DMAD盐酸盐抑制(0.1-500 μM;14小时;用Tg(0.3 μM)处理的HT1080细胞)[1]。 3,6-DMAD 盐酸盐(1-60 μM;2 小时;HEK293 细胞)可抑制 IRE1α 寡聚化和 IRE1α-GFP 灶的发育[1]。
|
---|---|
体内研究 (In Vivo) |
当给予 RPMI 8226 异种移植物的 NOD Scid 小鼠中给予 3,6-DMAD 盐酸盐(10 mg/kg;腹腔注射;每 12 小时 3 次,持续 84 小时)时,体内 XBP1 剪接受到抑制[1]。 3,6-DMAD 盐酸盐(10 mg/kg;24 小时;腹腔注射;每 48 小时一次,持续 12 天;NOD Scid 小鼠)可在体内抑制产生 RPMI 8226 异种移植物的多发性骨髓瘤异种移植物生长[1]。
|
细胞实验 |
细胞活力测定[1]
细胞类型: RPMI 8226 和 MM1.R 人类 MM 细胞 测试浓度: 0、0.5、1、2、3 、4、5 和 6 μM 孵育时间:24 小时 实验结果:以剂量依赖性方式抑制细胞存活率。 蛋白质印迹分析[1] 细胞类型:用 Tg(0.3 μM) 处理的 HT1080 细胞 测试浓度: 0, 5 、10 和 30 μM 孵育持续时间:14 小时 实验结果:证明在低至 0.5 μM 时即可抑制 XBP1s。 |
动物实验 |
Animal/Disease Models: NOD SCID (severe combined immunodeficient) mouse (4-6 weeks) with RPMI 8226 xenograft[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; three times every 12 hrs (hours), for 84 hrs (hours) Experimental Results: Inhibited XBP1-luciferase activity in NOD SCID (severe combined immunodeficient) mouse with RPMI 8226 xenograft. Animal/Disease Models: NOD SCID (severe combined immunodeficient) mouse (4 -6 weeks) with RPMI 8226 xenograft[1] Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; every 48 hrs (hours), for 12 days Experimental Results: Inhibited tumor growth in NOD SCID (severe combined immunodeficient) mouse with RPMI 8226 xenograft. |
参考文献 |
[1]. Jiang D, et, al. Acridine Derivatives as Inhibitors of the IRE1α-XBP1 Pathway Are Cytotoxic to Human Multiple Myeloma. Mol Cancer Ther. 2016 Sep;15(9):2055-65.
[2]. De SY, et, al. SHP-2 specific deletion in macrophages accelerates pathological cardiac hypertrophy through promoting IRE1α-XBP1s pathway regulated by IL-6 secretion. Research Article. 2022 May 3. |
分子式 |
C22H31N5
|
---|---|
相关CAS号 |
3,6-DMAD dihydrochloride;2226511-77-7
|
溶解度 (体外) |
DMSO :~25 mg/mL
|
---|---|
溶解度 (体内) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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。 |
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) 。