Vorasidenib (AG-881)

For research use only.

Catalog No.S8611

2 publications

Vorasidenib (AG-881) Chemical Structure

CAS No. 1644545-52-7

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

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

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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 MonHRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnrUO|IhcHK| Mm\oRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOEfNS{Bk\WyuczDlfJBz\XO|aX7nJJBNXlhvSVTINkBTOTRyUTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmemeubzDy[YFo\W62IHLhd4VlKGG|c3H5MEBKSzVyPECuNFXPxE1? NIDuSnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
TS603 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2nSblczKGi{cx?= NF7G[W5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTTOlA{KGOnbHzzJIhiemKxcnnu[{BKTEh{IGKxOFBSKG23dHHueEBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXy[4xwKHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVA9OC5yNd88US=> NFjPS4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
HT1080 MmHkRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4H3eFczKGi{cx?= NFOzOFJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUNVA5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXy[4xwKHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVA9OC5yNd88US=> NHz4Zo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
Sf9 MVfGeY5kfGmxbjDhd5NigQ>? NHXWVJIyKGi{ NF:xcZhKdmirYnn0bY9vKG:oIFjpd{11[WepZXSge4lt\CC2eYDlJGlFUDFiKIXub45wf25ib4Lp[4lvMS:ITFHHMZRi\2enZDDJSGgyKFJzM{LIJI12fGGwdDDo[ZRmem:maX3ldkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJIFl\Gm2aX;uJI9nKGGucHjhMWtIKG[xbHzve4VlKGK7IHTpZZBpd3Kjc3WgZY5lKHKnc3H6eZJqdiCjZHTpeIlwdiCjbnSgcYVie3W{ZXSgZYZ1\XJiNTDtbY5{KGmwIIDy[ZNmdmNuIFnDOVA9OC5yNd88US=> NYLZcZg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
Sf9 NYXBN5lvTnWwY4Tpc44h[XO|YYm= MVuxJIhz NE\KcpNKdmirYnn0bY9vKG:oIFjpd{11[WepZXSge4lt\CC2eYDlJGlFUDFiKIXub45wf25ib4Lp[4lvMS:ITFHHMZRi\2enZDDJSGgyKFJzM{LDJI12fGGwdDDo[ZRmem:maX3ldkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh[mWob4LlJIFl\Gm2aX;uJI9nKGGucHjhMWtIKG[xbHzve4VlKGK7IHTpZZBpd3Kjc3WgZY5lKHKnc3H6eZJqdiCjZHTpeIlwdiCjbnSgcYVie3W{ZXSgZYZ1\XJiNTDtbY5{KGmwIIDy[ZNmdmNuIFnDOVA9OC5yNd88US=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
Sf9 NH\iNFdHfW6ldHnvckBie3OjeR?= M334N|EhcHJ? NGDOWYVKdmirYnn0bY9vKG:oIFTINUBTOTN{SDDteZRidnRiaH;tc4RqdWW{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCjZHTpeIlwdiCxZjDhcJBp[S2NRzDmc4xtd3enZDDifUA3OCCvaX7zJIlv[3WkYYTpc44hcW5icILld4Vv[2Vib3[gUmFFWEhuIF7BSHAtKGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBjgSCobIXvdoV{[2WwY3Wgd5Bm[3S{b33leJJ6NCCLQ{WwQFAvODYQvF2= NVTR[|BiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
Sf9 MWHGeY5kfGmxbjDhd5NigQ>? NHezeZUyKGi{ NFLTW4ZKdmirYnn0bY9vKG:oIFTINUBTOTN{QzDteZRidnRiaH;tc4RqdWW{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BxemVvaX7jeYJifGWmIH\vdkAyKGi{IHLl[o9z\SCjZHTpeIlwdiCxZjDhcJBp[S2NRzDmc4xtd3enZDDifUA3OCCvaX7zJIlv[3WkYYTpc44hcW5icILld4Vv[2Vib3[gUmFFWEhuIF7BSHAtKGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBjgSCobIXvdoV{[2WwY3Wgd5Bm[3S{b33leJJ6NCCLQ{WwQFAvODYQvF2= NITKXXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 M3HlZmZ2dmO2aX;uJIF{e2G7 NUjGcY5MOSCqch?= MnXETY5pcWKrdHnvckBw\iCLRFiyJHIyPDCTIH31eIFvfCCqb33v[Ilu\XJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGGmZHn0bY9vKG:oIHHsdIhiNUuJIH\vcIxwf2WmIHL5JFE3KGi{czDpcoN2[mG2aX;uJIlvKHC{ZYPlcoNmKG:oIF7BSHBJNCCQQVTQMEBlcWGyaH;yZZNmKGGwZDDy[ZNignW{aX6gZpkh\my3b4Lld4NmdmOnIIPw[YN1em:vZYTyfUBj[XOnZDDjc4ZiNCCLQ{WwQFAvODYQvF2= MmfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
HT1080 Mn;qSpVv[3Srb36gZZN{[Xl? MVW0PEBpenN? NXfIcYVPUW6qaXLpeIlwdiCxZjDJSGgyKFJzM{LIM3IyOzKFIH31eIFvfCCrbjDoeY1idiCKVEGwPFAh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIEKtTGch\m:{bXH0bY9vKGmwY4XiZZRm\CCob4KgOFghcHK|IHL5JGxENU2VIH3leIhw\CxiSVO1NFwxNjB3zszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
U87MG M3W0XGZ2dmO2aX;uJIF{e2G7 NE\3bIE1QCCqcoO= Mnz6TY5pcWKrdHnvckBw\iCLRFixJHIyOzKFIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDoeY1idiCXOEfNS{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iMj3IS{Bnd3KvYYTpc44hcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUGMuVVNibXX0bI9lNCCLQ{WwQFAvODYQvF2= NGrYTFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
TS603 NYTucJFTTnWwY4Tpc44h[XO|YYm= NEH1[|c1QCCqcoO= M1fMcmlvcGmkaYTpc44hd2ZiRFixJHIyOzKKIH31eIFvfCCrbjDoeY1idiCWU{[wN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iMj3IS{Bnd3KvYYTpc44hcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUGMuVVNibXX0bI9lNCCLQ{WwQFAvODYQvF2= MlLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>

... Click to View More Cell Line Experimental Data

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

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 powder
in solvent
Synonyms N/A
Smiles CC(C(F)(F)F)NC1=NC(=NC(=N1)C2=NC(=CC=C2)Cl)NC(C)C(F)(F)F

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID