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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

Vorasidenib (AG-881) Chemical Structure

CAS: 1644545-52-7

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 3251.43 現(xiàn)貨
2mg 1286.44 現(xiàn)貨
5mg 2924.8 現(xiàn)貨
25mg 8763.8 現(xiàn)貨
100mg 17772.63 現(xiàn)貨
1g 33497.46 現(xiàn)貨
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Vorasidenib (AG-881)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Dehydrogenase Signaling Pathways

Dehydrogenase信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)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(diǎn)
IDH1 [1] IDH2 [1]
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(nèi)外模型中誘導(dǎo)細(xì)胞分化[1]。 AG-881抑制α-KG轉(zhuǎn)變成癌代謝物2HG，抑制2HG介導(dǎo)的信號(hào)、并引起細(xì)胞分化、表達(dá)突變型IDH的腫瘤細(xì)胞增殖受到抑制[2]。
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 AG-881可完全穿過(guò)血腦屏障。目前AG-881處于臨床早期I期試驗(yàn)，檢測(cè)其對(duì)治療具有IDH突變的惡性血液病、實(shí)體腫瘤、膠質(zhì)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(xué)信息&溶解度

分子量 414.74 分子式

C14H13ClF6N6
CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 82 mg/mL ( (197.71 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 82 mg/mL (197.71 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)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(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)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(nèi)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(jìn)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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