LLY-283
目录号 : GC33184A PRMT5 inhibitor
Cas No.:2040291-27-6
Sample solution is provided at 25 µL, 10mM.
LLY-283 is an inhibitor of protein arginine methyltransferase 5 (PRMT5; IC50 = 22 nM).1 It is selective for PRMT5 over a panel of methyltransferases, including PRMT4, -6, and -7 at 1 μM. It reduces symmetric demethylation of SmBB' in MCF-7 cells (IC50 = 25 nM) and inhibits proliferation of various breast, gastric, hematological, lung, skin, and ovarian cancer cell lines (IC50s = 3-30 nM). LLY-283 (20 mg/kg) inhibits tumor growth in an A375 mouse xenograft model. It also disrupts alternative splicing events in, and inhibits proliferation and self-renewal of, patient-derived glioblastoma stem cells and increases survival in an orthotopic patient-derived xenograft (PDX) mouse model.2 See the Structural Genomics Consortium (SGC) website for more information.
1.Bonday, Z.Q., Cortez, G.S., Grogan, M.J., et al.LLY-283, a potent and selective inhibitor of arginine methyltransferase 5, PRMT5, with antitumor activityACS Med. Chem. Lett.9(7)612-617(2018) 2.Sachamitr, P., Ho, J.C., Ciamponi, F.E., et al.PRMT5 inhibition disrupts splicing and stemness in glioblastomaNat. Commun.12(1)979(2021)
Cas No. | 2040291-27-6 | SDF | |
Canonical SMILES | O[C@H]1[C@@H](O[C@@]([C@@H](C2=CC=CC=C2)O)([H])[C@H]1O)N3C4=NC=NC(N)=C4C=C3 | ||
分子式 | C17H18N4O4 | 分子量 | 342.35 |
溶解度 | DMSO: 250 mg/mL (730.25 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 | 2.921 mL | 14.6049 mL | 29.2099 mL |
5 mM | 0.5842 mL | 2.921 mL | 5.842 mL |
10 mM | 0.2921 mL | 1.4605 mL | 2.921 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet