3,6-DMAD hydrochloride
目录号 : GC343843,6-DMADhydrochloride是未折叠蛋白质应答(IRE1α-XBP1)通路的抑制剂。
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | IRE1α oligomerization assay is set up using the nuclease reaction buffer, 2 μM recombinant hIRE1α, 2 mM ADP, and 60 μM of 3,6-DMAD. All reactions are performed in 20 μL with 10% DMSO to account for vehicle and incubated for 15 min at 30 °C to allow for oligomerization. The optical density of the sample is measured at 500 nm using a NanoDrop 2000[1]. |
Cell experiment: | 2×104 cells per well are plated into 96-well plates and treatment started 0-12 hours after plating. RPMI 8226 and MM1.R human MM cells are treated with 0-6 μM 3,6-DMAD. After 24 hours of treatment, XTT reagent (ATCC) is added to the wells then cells are incubated for 2 hours and absorbance measured at both 475 nM and 660 nM using a BioTek Synergy H1 plate reader.[1]. |
Animal experiment: | Rats[1]5×106RPMI 8226 cells are implanted subcutaneously into the flanks of 4-6 weeks’ old NOD Scid mice. Drug treatment started when the sizes of the tumors reach 150 mm3. Four tumor-bearing mice per group are treated with 10 mg/kg 3,6-DMAD or vehicle (saline) intraperitoneally once every 2 days. Tumor volume is measured[1]. |
References: [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. |
3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway of the unfolded protein response.
3,6-DMAD inhibits both IRE1α oligomerization and in vitro endoribonuclease (RNase) activity[1].
Following three intraperitoneal administrations of 3,6-DMAD at a dose of 10 mg/kg every 12 hours, 3,6-DMAD significantly inhibits in vivo XBP1-luciferase activity assessed 3.5 days after the initial treatment. 3,6-DMAD-treatment significantly inhibits tumor xenograft growth[1].
[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.
Cas No. | SDF | ||
Canonical SMILES | CN(C1=CC=C2C(N=C3C=C(C=CC3=C2NCCCN(C)C)N(C)C)=C1)C.[x HCl] | ||
分子式 | C22H31N5 xHCl | 分子量 | 365.52 |
溶解度 | DMSO : 25 mg/mL (68.40 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7358 mL | 13.6791 mL | 27.3583 mL |
5 mM | 0.5472 mL | 2.7358 mL | 5.4717 mL |
10 mM | 0.2736 mL | 1.3679 mL | 2.7358 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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,
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 saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。