PF-06939999 (hydrochloride)
(Synonyms: PRMT5-IN-3; PRMT5 Inhibitor 3; Protein Arginine Methyltransferase 5-IN-3; Protein Arginine Methyltransferase 5 Inhibitor 3) 目录号 : GC92688PF-06939999 is an inhibitor of protein arginine metltransferase 5 (PRMT5; Ki = <5 pM).
Sample solution is provided at 25 µL, 10mM.
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PF-06939999 is an inhibitor of protein arginine metltransferase 5 (PRMT5; Ki = ＜5 pM). It is selective for PRMT5 over a panel of 22 additional protein metltransferases and a panel of 40 kinases at 10 µM. PF-06939999 decreases global symmetric dimetl arginine levels (IC50 = 1.1 nM) but does not affect histone metlation levels in A-427 non-small cell lung cancer (NSCLC) cells. In vivo, PF-06939999 (3, 10, and 30 mg/kg) reduces tumor volume in an A-427 mouse xenograft model.
| Cas No. | SDF | ||
| 别名 | PRMT5-IN-3; PRMT5 Inhibitor 3; Protein Arginine Methyltransferase 5-IN-3; Protein Arginine Methyltransferase 5 Inhibitor 3 | ||
| 化学名 | (1S,2S,3S,5R)-3-[[6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydro-8-isoquinolinyl]oxy]-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-1,2-cyclopentanediol, dihydrochloride | ||
| Canonical SMILES | O[C@H]1[C@@H](C[C@@H]([C@H]1O)OC2=C3C(CCNC3)=C(C(C(F)F)=C2)F)N4C5=NC=NC(C)=C5C=C4.Cl.Cl | ||
| 分子式 | C22H23F3N4O3 • 2HCl | 分子量 | 521.3 |
| 溶解度 | Acetonitrile: Slightly soluble: 0.1-1 mg/ml; Water: Slightly soluble: 0.1-1 mg/ml | 储存条件 | -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9183 mL | 9.5914 mL | 19.1828 mL |
| 5 mM | 383.7 μL | 1.9183 mL | 3.8366 mL |
| 10 mM | 191.8 μL | 959.1 μL | 1.9183 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet