AG-120
(Synonyms: 艾伏尼布,AG-120) 目录号 : GC15601
An IDH1 inhibitor
Cas No.:1448347-49-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: < 100 nM
AG-120 is an IDH1 inhibitor.
Isocitrate dehydrogenase (IDH) is a metabolic enzyme interconverting isocitrate and α-ketoglutarate (α-KG), but cancer-associated mutations of IDH1 and IDH2 confer a neomorphic activity, which allows reduction of α-KG to the oncometabolite 2-HG.
In vitro: TF-1 cells or primary human AML patient samples expressing mutant IDH1 were treated with AG-120, and the results showed that in TF-1 IDH1-R132H cells, AG-120 was able to decrease the intracellular 2-HG levels, inhibit growth factor independent proliferation and restore erythropoietin-induced differentiation [1].
Ex vivo: Previous ex-vivo study showed that the pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells led to an effective way to lower intracellular 2-HG levels and induced myeloid differentiation [1].
Clinical trial: In a phase I clinical trial, 62 patients with advanced IDH1 mutation–positive solid tumors were treated with single agent AG-120 orally once a day. Results showed that 7 of 11 patients with IDH1 mutant–positive chondrosarcoma had stable disease; 1 out of 20 patients with IDH1 mutant–positive IHCC had a partial response and 11 patients had SD; and one out of four patients with other IDH1 mutant–positive solid tumors had SD [2].
References:
[1] Erica Hansen et al. AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples Treated Ex Vivo. Blood 2014 124:3734.
[2] http://www. aacr.org/Newsroom/Pages/News-Release-Detail.aspx ItemID=789#.WLAUOm997IU
| Cas No. | 1448347-49-6 | SDF | |
| 别名 | 艾伏尼布,AG-120 | ||
| 化学名 | (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide | ||
| Canonical SMILES | O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5 | ||
| 分子式 | C28H22ClF3N6O3 | 分子量 | 582.96 |
| 溶解度 | ≥ 58.3mg/mL in DMSO | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7154 mL | 8.5769 mL | 17.1538 mL |
| 5 mM | 0.3431 mL | 1.7154 mL | 3.4308 mL |
| 10 mM | 0.1715 mL | 0.8577 mL | 1.7154 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。