Vorasidenib (AG-881)

目录号:S8611

仅限科研使用

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

规格 价格 库存 购买数量
RMB 1286.44 现货
RMB 2924.8 现货
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客户使用Selleck生产的Vorasidenib (AG-881)发表文献2篇:

产品安全说明书

Dehydrogenase抑制剂选择性比较

相关Dehydrogenase产品

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG M3jMb2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1vpbVczKGi{cx?= MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV6N13HJINmdGy|IHX4dJJme3OrbnegdGxXYC2LRFiyJHIyPDCTIH31eIFvfCCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVz\2yxIILlZYdmdnRiYnHz[YQh[XO|YYmsJGlEPTB:MD6wOe69VQ>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh2N{mzNEc,Ojl6NEe5N|A9N2F-
TS603 MkW5RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4[xfFczKGi{cx?= M4\kZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVGO2NFMh[2WubIOgbIFz[m:{aX7nJGlFUDJiUkG0NHEhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYLncI8hemWjZ3XueEBj[XOnZDDhd5NigSxiSVO1NFwxNjB3zszN M{e5WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OES3PVMxLz5{OUi0O|k{ODxxYU6=
HT1080 MWHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NEHEWGQ4OiCqcoO= MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWMUC4NEBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{Z3zvJJJm[WenboSgZoF{\WRiYYPzZZktKEmFNUC8NE4xPc7:TR?= NI[zcII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
Sf9 MXHGeY5kfGmxbjDhd5NigQ>? NVLO[Jd{OSCqch?= MWjJcohq[mm2aX;uJI9nKEircz30ZYdo\WRid3ns[EB1gXCnIFnETFEhMHWwa37ve44hd3KrZ3nuLU9HVEGJLYTh[4dm\CCLRFixJHIyOzKKIH31eIFvfCCqZYTldo9lcW2ncjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHC{ZT3pcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIHHk[Il1cW:wIH;mJIFteGijLVvHJIZwdGyxd3XkJIJ6KGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBi\GSrdHnvckBidmRibXXhd5Vz\WRiYX\0[ZIhPSCvaX7zJIlvKHC{ZYPlcoMtKEmFNUC8NE4xPc7:TR?= MmnXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
Sf9 NUfpdYs1TnWwY4Tpc44h[XO|YYm= MXuxJIhz MnHoTY5pcWKrdHnvckBw\iCKaYOteIFo\2WmIIfpcIQhfHmyZTDJSGgyKCi3bnvuc5dvKG:{aXfpckkwTkyDRz30ZYdo\WRiSVTINUBTOTN{QzDteZRidnRiaHX0[ZJw\GmvZYKg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyCycnWtbY5kfWKjdHXkJIZweiBzIHjyJIJm\m:{ZTDh[IRqfGmxbjDv[kBidHCqYT3LS{Bnd2yub4fl[EBjgSCmaXHwbI9z[XOnIHHu[EBz\XOjeoXybY4h[WSmaYTpc44h[W6mIH3lZZN2emWmIHHmeIVzKDVibXnud{BqdiCycnXz[Y5kNCCLQ{WwQFAvODYQvF2= MoTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
Sf9 MmLhSpVv[3Srb36gZZN{[Xl? MX:xJIhz M4TQfmlvcGmkaYTpc44hd2ZiRFixJHIyOzKKIH31eIFvfCCqb33v[Ilu\XJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGGmZHn0bY9vKG:oIHHsdIhiNUuJIH\vcIxwf2WmIHL5JFYxKG2rboOgbY5kfWKjdHnvckBqdiCycnXz[Y5k\SCxZjDORWRRUCxiTlHEVEwh\GmjcHjvdoF{\SCjbnSgdoV{[Xq3cnnuJIJ6KG[udX;y[ZNk\W6lZTDzdIVkfHKxbXX0dpktKEmFNUC8NE4xPc7:TR?= NGO5d4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 MVnGeY5kfGmxbjDhd5NigQ>? NGCzXFYyKGi{ NXfuWm9JUW6qaXLpeIlwdiCxZjDETFEhWjF|MlOgcZV1[W62IHjvcY9lcW2ncjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBU\jliY3XscJMheHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViYXTkbZRqd25ib3[gZYxxcGFvS1eg[o9tdG:5ZXSgZpkhPjBibXnud{BqdmO3YnH0bY9vKGmwIIDy[ZNmdmOnIH;mJG5CTFCKLDDORWRRNCCmaXHwbI9z[XOnIHHu[EBz\XOjeoXybY4h[nliZnz1c5Jme2OnbnPlJJNx\WO2cn;t[ZRzgSxiSVO1NFwxNjB3zszN MmTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
Sf9 NGX6PFVHfW6ldHnvckBie3OjeR?= MnnvNUBpeg>? NEXHR2ZKdmirYnn0bY9vKG:oIFnETFIhWjF2MGGgcZV1[W62IHjvcY9lcW2ncjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBU\jliY3XscJMheHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViYXTkbZRqd25ib3[gZYxxcGFvS1eg[o9tdG:5ZXSgZpkhOTZiaILzJIlv[3WkYYTpc44hcW5icILld4Vv[2Vib3[gUmFFWEhuIF7BSHAtKGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBjgSCobIXvdoV{[2WwY3Wgd5Bm[3S{b33leJJ6KGKjc3XkJINw\mFuIFnDOVA9OC5yNd88US=> NUX2[2F5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
HT1080 NHTHV4VHfW6ldHnvckBie3OjeR?= NWnaZ4F5PDhiaILz Mkf5TY5pcWKrdHnvckBw\iCLRFixJHIyOzKKL2KxN|JEKG23dHHueEBqdiCqdX3hckBJXDFyOECgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKDJvSFeg[o9zdWG2aX;uJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IFzDMW1UKG2ndHjv[EwhUUN3MEywMlA2|ryP NFS5[WI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
U87MG M{L1[GZ2dmO2aX;uJIF{e2G7 MUK0PEBpenN? NF;Ze3NKdmirYnn0bY9vKG:oIFnETFEhWjF|MlOgcZV1[W62IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIGW4O21IKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjCyMWhIKG[xcn3heIlwdiCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBNSy2PUzDt[ZRpd2RuIFnDOVA9OC5yNd88US=> M4fHPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
TS603 NWjzO2Z7TnWwY4Tpc44h[XO|YYm= MXS0PEBpenN? NUH0Z|JTUW6qaXLpeIlwdiCxZjDETFEhWjF|MligcZV1[W62IHnuJIh2dWGwIGTTOlA{KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjCyMWhIKG[xcn3heIlwdiCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBNSy2PUzDt[ZRpd2RuIFnDOVA9OC5yNd88US=> M1y0OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度(25°C)

体外

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 414.74
化学式

C14H13ClF6N6

CAS号 1644545-52-7
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04164901 Active not recruiting Drug: Vorasidenib|Drug: Matching Placebo Grade 2 Glioma|Residual Glioma|Recurrent Glioma Institut de Recherches Internationales Servier|Servier January 5 2020 Phase 3
NCT04145128 Completed Drug: AG881 Healthy Volunteers Agios Pharmaceuticals Inc. October 2 2019 Phase 1
NCT04015687 Completed Drug: AG-881|Drug: Lamotrigine Healthy Participants Agios Pharmaceuticals Inc. July 15 2019 Phase 1
NCT03960502 Completed Drug: AG-881|Drug: [13C315N3]AG-881 Healthy Male Participants Agios Pharmaceuticals Inc. May 16 2019 Phase 1
NCT03343197 Active not recruiting Drug: AG-120|Drug: AG881 Glioma Institut de Recherches Internationales Servier|Servier March 20 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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