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

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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 MX3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2fselczKGi{cx?= MoHFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOEfNS{Bk\WyuczDlfJBz\XO|aX7nJJBNXlhvSVTINkBTOTRyUTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmemeubzDy[YFo\W62IHLhd4VlKGG|c3H5MEBKSzVyPECuNFXPxE1? M4[5S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OES3PVMxLz5{OUi0O|k{ODxxYU6=
TS603 MnnTRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NETISo04OiCqcoO= MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSVNkCzJINmdGy|IHjhdoJwemmwZzDJSGgzKFJzNEDRJI12fGGwdDDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{Z3zvJJJm[WenboSgZoF{\WRiYYPzZZktKEmFNUC8NE4xPc7:TR?= NIm5O3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
HT1080 M2XHWGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mn\TO|IhcHK| NELJdWVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUNVA5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXy[4xwKHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVA9OC5yNd88US=> NGjCUXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
Sf9 M1iwbWZ2dmO2aX;uJIF{e2G7 NIfifHAyKGi{ MX\Jcohq[mm2aX;uJI9nKEircz30ZYdo\WRid3ns[EB1gXCnIFnETFEhMHWwa37ve44hd3KrZ3nuLU9HVEGJLYTh[4dm\CCLRFixJHIyOzKKIH31eIFvfCCqZYTldo9lcW2ncjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHC{ZT3pcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIHHk[Il1cW:wIH;mJIFteGijLVvHJIZwdGyxd3XkJIJ6KGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBi\GSrdHnvckBidmRibXXhd5Vz\WRiYX\0[ZIhPSCvaX7zJIlvKHC{ZYPlcoMtKEmFNUC8NE4xPc7:TR?= MlnCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
Sf9 Moe0SpVv[3Srb36gZZN{[Xl? NFvMPIgyKGi{ NVjYUpk6UW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJJdqdGRidInw[UBKTEhzIDj1cotvd3ewIH;ybYdqdilxRlzBS{11[WepZXSgTWRJOSCUMUOyR{BufXSjboSgbIV1\XKxZHnt[ZIh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjCxJIhzKGKnZn;y[UBi\GSrdHnvckBw\iCjbIDoZU1MTyCob3zsc5dm\CCkeTDkbYFxcG:{YYPlJIFv\CC{ZYPhfpVzcW5iYXTkbZRqd25iYX7kJI1m[XO3cnXkJIFnfGW{IEWgcYlveyCrbjDwdoV{\W6lLDDJR|UxRDBwMEZOwG0> NF\2NHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 M17Wb2Z2dmO2aX;uJIF{e2G7 NFnlNIEyKGi{ MnvETY5pcWKrdHnvckBw\iCGSEGgVlE{OkhibYX0ZY51KGixbX;kbY1meiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgdJJmNWmwY4XiZZRm\CCob4KgNUBpeiCkZX\vdoUh[WSmaYTpc44hd2ZiYXzwbIEuU0diZn;scI94\WRiYomgOlAhdWmwczDpcoN2[mG2aX;uJIlvKHC{ZYPlcoNmKG:oIF7BSHBJNCCQQVTQMEBlcWGyaH;yZZNmKGGwZDDy[ZNignW{aX6gZpkh\my3b4Lld4NmdmOnIIPw[YN1em:vZYTyfUwhUUN3MEywMlA2|ryP NUDv[mJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
Sf9 NVX5RYxxTnWwY4Tpc44h[XO|YYm= M3\jPFEhcHJ? NUnqVJZkUW6qaXLpeIlwdiCxZjDETFEhWjF|MlOgcZV1[W62IHjvcY9lcW2ncjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBU\jliY3XscJMheHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViYXTkbZRqd25ib3[gZYxxcGFvS1eg[o9tdG:5ZXSgZpkhPjBibXnud{BqdmO3YnH0bY9vKGmwIIDy[ZNmdmOnIH;mJG5CTFCKLDDORWRRNCCmaXHwbI9z[XOnIHHu[EBz\XOjeoXybY4h[nliZnz1c5Jme2OnbnPlJJNx\WO2cn;t[ZRzgSxiSVO1NFwxNjB3zszN M{fBXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
Sf9 NHjWWIxHfW6ldHnvckBie3OjeR?= M2nETlEhcHJ? MnjBTY5pcWKrdHnvckBw\iCLRFiyJHIyPDCTIH31eIFvfCCqb33v[Ilu\XJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGGmZHn0bY9vKG:oIHHsdIhiNUuJIH\vcIxwf2WmIHL5JFE3KGi{czDpcoN2[mG2aX;uJIlvKHC{ZYPlcoNmKG:oIF7BSHBJNCCQQVTQMEBlcWGyaH;yZZNmKGGwZDDy[ZNignW{aX6gZpkh\my3b4Lld4NmdmOnIIPw[YN1em:vZYTyfUBj[XOnZDDjc4ZiNCCLQ{WwQFAvODYQvF2= M{jQR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
HT1080 Mn;3SpVv[3Srb36gZZN{[Xl? NIjrUJA1QCCqcoO= MmHuTY5pcWKrdHnvckBw\iCLRFixJHIyOzKKL2KxN|JEKG23dHHueEBqdiCqdX3hckBJXDFyOECgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKDJvSFeg[o9zdWG2aX;uJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IFzDMW1UKG2ndHjv[EwhUUN3MEywMlA2|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
U87MG MX7GeY5kfGmxbjDhd5NigQ>? NIj4TmI1QCCqcoO= NXvJfYpmUW6qaXLpeIlwdiCxZjDJSGgyKFJzM{LDJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBpfW2jbjDVPFdOTyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gNk1JTyCob4LtZZRqd25iaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVENvTWOgcYV1cG:mLDDJR|UxRDBwMEZOwG0> M33sflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
TS603 NGW5S41HfW6ldHnvckBie3OjeR?= NXPKR2FQPDhiaILz MUfJcohq[mm2aX;uJI9nKESKMTDSNVMzUCCvdYThcpQhcW5iaIXtZY4hXFN4MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKDJvSFeg[o9zdWG2aX;uJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IFzDMW1UKG2ndHjv[EwhUUN3MEywMlA2|ryP NYXmfI9QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDJ5OUC0O{8oRkOqRV3CUFww[T5?
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

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)

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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 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 2022-01-17)

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