Vorasidenib (AG-881)

Catalog No.S8611

For research use only.

Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).

Vorasidenib (AG-881) Chemical Structure

CAS No. 1644545-52-7

Selleck's Vorasidenib (AG-881) has been cited by 2 Publications

Purity & Quality Control

Choose Selective Dehydrogenase Inhibitors

Other Dehydrogenase Products

Biological Activity

Description Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).
Targets
IDH1 [1]
()
IDH2 [1]
()
In vitro

Pan-IDH1/2 inhibitor (AG881) selectively inhibit mutant IDH protein and induce cell differentiation in in vitro and in vivo models[1]. Upon administration, pan-IDH mutant inhibitor AG-881 specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG Mn;oRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3i5bVczKGi{cx?= MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV6N13HJINmdGy|IHX4dJJme3OrbnegdGxXYC2LRFiyJHIyPDCTIH31eIFvfCCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVz\2yxIILlZYdmdnRiYnHz[YQh[XO|YYmsJGlEPTB:MD6wOe69VQ>? M136NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OES3PVMxLz5{OUi0O|k{ODxxYU6=
TS603 NXfZOIVPSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3rPPFczKGi{cx?= NFXkTHdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTTOlA{KGOnbHzzJIhiemKxcnnu[{BKTEh{IGKxOFBSKG23dHHueEBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXy[4xwKHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVA9OC5yNd88US=> M3zQdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OES3PVMxLz5{OUi0O|k{ODxxYU6=
HT1080 NESwPHlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NWnkcFVpPzJiaILz M{fGRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGSxNFgxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYLncI8hemWjZ3XueEBj[XOnZDDhd5NigSxiSVO1NFwxNjB3zszN M3\Cc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OES3PVMxLz5{OUi0O|k{ODxxYU6=
Sf9 MYfGeY5kfGmxbjDhd5NigQ>? MlHCNUBpeg>? NY\Gd3M6UW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJJdqdGRidInw[UBKTEhzIDj1cotvd3ewIH;ybYdqdilxRlzBS{11[WepZXSgTWRJOSCUMUOyTEBufXSjboSgbIV1\XKxZHnt[ZIh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjCxJIhzKGKnZn;y[UBi\GSrdHnvckBw\iCjbIDoZU1MTyCob3zsc5dm\CCkeTDkbYFxcG:{YYPlJIFv\CC{ZYPhfpVzcW5iYXTkbZRqd25iYX7kJI1m[XO3cnXkJIFnfGW{IEWgcYlveyCrbjDwdoV{\W6lLDDJR|UxRDBwMEZOwG0> NHXwXnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 M{nqV2Z2dmO2aX;uJIF{e2G7 MUSxJIhz NVzlfmV1UW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJJdqdGRidInw[UBKTEhzIDj1cotvd3ewIH;ybYdqdilxRlzBS{11[WepZXSgTWRJOSCUMUOyR{BufXSjboSgbIV1\XKxZHnt[ZIh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjCxJIhzKGKnZn;y[UBi\GSrdHnvckBw\iCjbIDoZU1MTyCob3zsc5dm\CCkeTDkbYFxcG:{YYPlJIFv\CC{ZYPhfpVzcW5iYXTkbZRqd25iYX7kJI1m[XO3cnXkJIFnfGW{IEWgcYlveyCrbjDwdoV{\W6lLDDJR|UxRDBwMEZOwG0> NWW0VJJFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
Sf9 Mlr5SpVv[3Srb36gZZN{[Xl? M2XxdlEhcHJ? NHvONZNKdmirYnn0bY9vKG:oIFTINUBTOTN{SDDteZRidnRiaH;tc4RqdWW{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCjZHTpeIlwdiCxZjDhcJBp[S2NRzDmc4xtd3enZDDifUA3OCCvaX7zJIlv[3WkYYTpc44hcW5icILld4Vv[2Vib3[gUmFFWEhuIF7BSHAtKGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBjgSCobIXvdoV{[2WwY3Wgd5Bm[3S{b33leJJ6NCCLQ{WwQFAvODYQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
Sf9 MYLGeY5kfGmxbjDhd5NigQ>? NF\ERWUyKGi{ NHW1[3pKdmirYnn0bY9vKG:oIFTINUBTOTN{QzDteZRidnRiaH;tc4RqdWW{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCjZHTpeIlwdiCxZjDhcJBp[S2NRzDmc4xtd3enZDDifUA3OCCvaX7zJIlv[3WkYYTpc44hcW5icILld4Vv[2Vib3[gUmFFWEhuIF7BSHAtKGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBjgSCobIXvdoV{[2WwY3Wgd5Bm[3S{b33leJJ6NCCLQ{WwQFAvODYQvF2= NUjIbHdKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
Sf9 NEPTXpZHfW6ldHnvckBie3OjeR?= NFrxd5IyKGi{ MlSwTY5pcWKrdHnvckBw\iCLRFiyJHIyPDCTIH31eIFvfCCqb33v[Ilu\XJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGGmZHn0bY9vKG:oIHHsdIhiNUuJIH\vcIxwf2WmIHL5JFE3KGi{czDpcoN2[mG2aX;uJIlvKHC{ZYPlcoNmKG:oIF7BSHBJNCCQQVTQMEBlcWGyaH;yZZNmKGGwZDDy[ZNignW{aX6gZpkh\my3b4Lld4NmdmOnIIPw[YN1em:vZYTyfUBj[XOnZDDjc4ZiNCCLQ{WwQFAvODYQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
HT1080 NGnBfWpHfW6ldHnvckBie3OjeR?= M3K0RlQ5KGi{cx?= MXfJcohq[mm2aX;uJI9nKEmGSEGgVlE{OkhxUkGzNmMhdXW2YX70JIlvKGi3bXHuJGhVOTB6MDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hOi2KRzDmc5Ju[XSrb36gbY5kfWKjdHXkJIZweiB2ODDodpMh[nliTFOtUXMhdWW2aH;kMEBKSzVyPECuNFXPxE1? M4frR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
U87MG NUHTNFN5TnWwY4Tpc44h[XO|YYm= NUCxcpFYPDhiaILz NXf5dVZ3UW6qaXLpeIlwdiCxZjDJSGgyKFJzM{LDJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBpfW2jbjDVPFdOTyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gNk1JTyCob4LtZZRqd25iaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVENvTWOgcYV1cG:mLDDJR|UxRDBwMEZOwG0> NYjHUnR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
TS603 NVjoS2pwTnWwY4Tpc44h[XO|YYm= MlXlOFghcHK| MWDJcohq[mm2aX;uJI9nKESKMTDSNVMzUCCvdYThcpQhcW5iaIXtZY4hXFN4MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKDJvSFeg[o9zdWG2aX;uJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IFzDMW1UKG2ndHjv[EwhUUN3MEywMlA2|ryP NHjQNZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
In vivo AG-881 fully penetrates the blood-brain barrier. AG-881 has been developed and is in early phase I testing for patients with IDH mutation-positive hematologic malignancies and solid tumors, including glioma[3].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 82 mg/mL
(197.71 mM)
Ethanol 82 mg/mL
(197.71 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 414.74
Formula

C14H13ClF6N6

CAS No. 1644545-52-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(F)(F)F)NC1=NC(=NC(=N1)C2=NC(=CC=C2)Cl)NC(C)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04164901 Recruiting Drug: Vorasidenib|Drug: Matching Placebo Grade 2 Glioma|Residual Glioma|Recurrent Glioma Agios Pharmaceuticals Inc. 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 2021-09-06)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Vorasidenib|Vorasidenib ic50|Vorasidenib price|Vorasidenib cost|Vorasidenib solubility dmso|Vorasidenib purchase|Vorasidenib manufacturer|Vorasidenib research buy|Vorasidenib order|Vorasidenib mouse|Vorasidenib chemical structure|Vorasidenib mw|Vorasidenib molecular weight|Vorasidenib datasheet|Vorasidenib supplier|Vorasidenib in vitro|Vorasidenib cell line|Vorasidenib concentration|Vorasidenib nmr|Vorasidenib in vivo|Vorasidenib clinical trial|Vorasidenib inhibitor|Vorasidenib Metabolism inhibitor