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

Vorasidenib (AG-881) Chemical Structure

CAS: 1644545-52-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3251.43 现货
2mg RMB 1286.44 现货
5mg RMB 2924.8 现货
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客户使用Selleck的发表文献4

产品质控

批次: S861101 DMSO] 82 mg/mL] false] Ethanol] 82 mg/mL] false] Water] Insoluble] false 纯度: 99.99%
99.99

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
IDH1 [1] IDH2 [1]
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)

体外溶解度
批次:

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

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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,: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: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: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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