Vorasidenib (AG-881)
Vorasidenib (AG-881)是一種具有口服活性的抑制劑，靶向突變型IDH1和IDH2。
Vorasidenib (AG-881) Chemical Structure
CAS: 1644545-52-7
產品質控
批次：
純度：
99.99%
99.99
Vorasidenib (AG-881)相關產品
相關信號通路圖
細胞實驗數據示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | |
| 點擊查看更多細胞系數據 | |||||
生物活性
| 產品描述 | Vorasidenib (AG-881)是一種具有口服活性的抑制劑，靶向突變型IDH1和IDH2。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 泛IDH1/2抑制劑（AG881）選擇性地抑制突變型IDH蛋白，并在體內外模型中誘導細胞分化[1]。 AG-881抑制α-KG轉變成癌代謝物2HG，抑制2HG介導的信號、并引起細胞分化、表達突變型IDH的腫瘤細胞增殖受到抑制[2]。 | |||
|---|---|---|---|---|
| 體內研究(In Vivo) | ||
| 體內研究活性 | AG-881可完全穿過血腦屏障。目前AG-881處于臨床早期I期試驗，檢測其對治療具有IDH突變的惡性血液病、實體腫瘤、膠質瘤的效果[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 |
June 2024 | Phase 1 |
| NCT05674474 | Completed | 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 |
化學信息&溶解度
| 分子量 | 414.74 | 分子式 | C14H13ClF6N6 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 82 mg/mL ( (197.71 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 82 mg/mL (197.71 mM) Water : Insoluble |
摩爾濃度計算器 |
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體內溶解度 現配現用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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