Vorasidenib (AG-881)
Vorasidenib (AG-881)是一种具有口服活性的抑制剂，靶向突变型IDH1和IDH2。
Vorasidenib (AG-881) Chemical Structure
CAS: 1644545-52-7
客户使用Selleck的发表文献4篇
产品质控
Vorasidenib (AG-881)相关产品
相关信号通路图
Dehydrogenase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| TS603 | Function assay | 48 hrs | Inhibition of DH1 R132H mutant in human TS603 cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method, IC50<0.05μM | ChEMBL | |
| U87MG | Function assay | 48 hrs | Inhibition of IDH1 R132C mutant (unknown origin) expressed in human U87MG cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method, IC50<0.05μM | ChEMBL | |
| HT1080 | Function assay | 48 hrs | Inhibition of IDH1 R132H/R132C mutant in human HT1080 cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method, IC50<0.05μM | ChEMBL | |
| Sf9 | Function assay | 1 hr | Inhibition of IDH2 R140Q mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 16 hrs incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry based cofa, IC50<0.05μM | ChEMBL | |
| Sf9 | Function assay | 1 hr | Inhibition of DH1 R132C mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 60 mins incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry, IC50<0.05μM | ChEMBL | |
| Sf9 | Function assay | 1 hr | Inhibition of DH1 R132H mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 60 mins incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry, IC50<0.05μM | ChEMBL | |
| Sf9 | Function assay | 1 hr | Inhibition of His-tagged wild type IDH1 (unknown origin)/FLAG-tagged IDH1 R132C mutant heterodimer expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by diaphorase and resazurin addition and measured after 5 mins in presenc, IC50<0.05μM | ChEMBL | |
| HT1080 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT1080 cells after 72 hrs by celltiterglo reagent based assay, IC50<0.05μM | 29847930 | |
| Sf9 | Function assay | 1 hr | Inhibition of His-tagged wild type IDH1 (unknown origin)/FLAG-tagged IDH1 R132H mutant heterodimer expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by diaphorase and resazurin addition and measured after 5 mins in presenc, IC50<0.05μM | ChEMBL | |
| TS603 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human TS603 cells harboring IDH2 R140Q mutant after 72 hrs by celltiterglo reagent based assay, IC50<0.05μM | 29847930 | |
| U87MG | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U87MG cells expressing pLVX-IDH2 R140Q mutant after 72 hrs by celltiterglo reagent based assay, IC50<0.05μM | 29847930 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Vorasidenib (AG-881)是一种具有口服活性的抑制剂，靶向突变型IDH1和IDH2。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 泛IDH1/2抑制剂（AG881）选择性地抑制突变型IDH蛋白，并在体内外模型中诱导细胞分化[1]。 AG-881抑制α-KG转变成癌代谢物2HG，抑制2HG介导的信号、并引起细胞分化、表达突变型IDH的肿瘤细胞增殖受到抑制[2]。 | |||
|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | AG-881可完全穿过血脑屏障。目前AG-881处于临床早期I期试验，检测其对治疗具有IDH突变的恶性血液病、实体肿瘤、胶质瘤的效果[3]。 | |
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05609994 | Not yet recruiting | Low Grade Glioma of Brain |
Katy Peters MD PhD|Servier|Duke University |
February 2024 | Phase 1 |
| NCT05674474 | Recruiting | Hepatic Impairment |
Institut de Recherches Internationales Servier|Servier |
March 14 2023 | Phase 1 |
| NCT05484622 | Recruiting | Astrocytoma |
Institut de Recherches Internationales Servier|Merck Sharp & Dohme LLC|Servier |
January 20 2023 | Phase 1 |
| NCT04145128 | Completed | Healthy Volunteers |
Agios Pharmaceuticals Inc. |
October 2 2019 | Phase 1 |
化学信息&溶解度
| 分子量 | 414.74 | 分子式 | C14H13ClF6N6 |
| CAS号 | 1644545-52-7 | SDF | Download Vorasidenib (AG-881) SDF |
| Smiles | CC(C(F)(F)F)NC1=NC(=NC(=N1)C2=NC(=CC=C2)Cl)NC(C)C(F)(F)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 82 mg/mL ( (197.71 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 82 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
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Selleck为您提供正确的澄清溶液配方）
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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。
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