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 MULBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4[4[FczKGi{cx?= M{K2cWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVUi3UWch[2WubIOg[ZhxemW|c3nu[{BxVF[[LVnETFIhWjF2MGGgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSClZXzseIl1\XKpbH:gdoVi\2WwdDDiZZNm\CCjc4PhfUwhUUN3MEywMlA2|ryP NFHURWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUi0O|k{OCd-Mkm4OFc6OzB:L3G+
TS603 NWjpOm5ZSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MW[3NkBpenN? NH:3W2xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTTOlA{KGOnbHzzJIhiemKxcnnu[{BKTEh{IGKxOFBSKG23dHHueEBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXy[4xwKHKnYXflcpQh[mG|ZXSgZZN{[XluIFnDOVA9OC5yNd88US=> MlrQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NEe5N|AoRjJ7OES3PVMxRC:jPh?=
HT1080 NWDWOWpnSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NHz6SnA4OiCqcoO= M3HLRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGSxNFgxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYLncI8hemWjZ3XueEBj[XOnZDDhd5NigSxiSVO1NFwxNjB3zszN MkjwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6NEe5N|AoRjJ7OES3PVMxRC:jPh?=
Sf9 MmDhSpVv[3Srb36gZZN{[Xl? MUixJIhz MX;Jcohq[mm2aX;uJI9nKEircz30ZYdo\WRid3ns[EB1gXCnIFnETFEhMHWwa37ve44hd3KrZ3nuLU9HVEGJLYTh[4dm\CCLRFixJHIyOzKKIH31eIFvfCCqZYTldo9lcW2ncjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHC{ZT3pcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIHHk[Il1cW:wIH;mJIFteGijLVvHJIZwdGyxd3XkJIJ6KGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBi\GSrdHnvckBidmRibXXhd5Vz\WRiYX\0[ZIhPSCvaX7zJIlvKHC{ZYPlcoMtKEmFNUC8NE4xPc7:TR?= NFyyXVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 Mkm3SpVv[3Srb36gZZN{[Xl? M3jXUVEhcHJ? MnvZTY5pcWKrdHnvckBw\iCKaYOteIFo\2WmIIfpcIQhfHmyZTDJSGgyKCi3bnvuc5dvKG:{aXfpckkwTkyDRz30ZYdo\WRiSVTINUBTOTN{QzDteZRidnRiaHX0[ZJw\GmvZYKg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyCycnWtbY5kfWKjdHXkJIZweiBzIHjyJIJm\m:{ZTDh[IRqfGmxbjDv[kBidHCqYT3LS{Bnd2yub4fl[EBjgSCmaXHwbI9z[XOnIHHu[EBz\XOjeoXybY4h[WSmaYTpc44h[W6mIH3lZZN2emWmIHHmeIVzKDVibXnud{BqdiCycnXz[Y5kNCCLQ{WwQFAvODYQvF2= NIH2Omc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 MXPGeY5kfGmxbjDhd5NigQ>? NWLyOHBTOSCqch?= M4nISmlvcGmkaYTpc44hd2ZiRFixJHIyOzKKIH31eIFvfCCqb33v[Ilu\XJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFEhcHJiYnXmc5JmKGGmZHn0bY9vKG:oIHHsdIhiNUuJIH\vcIxwf2WmIHL5JFYxKG2rboOgbY5kfWKjdHnvckBqdiCycnXz[Y5k\SCxZjDORWRRUCxiTlHEVEwh\GmjcHjvdoF{\SCjbnSgdoV{[Xq3cnnuJIJ6KG[udX;y[ZNk\W6lZTDzdIVkfHKxbXX0dpktKEmFNUC8NE4xPc7:TR?= M1v1eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQzPzlyNEevK|5EcEWPQly8M4E,
Sf9 MVLGeY5kfGmxbjDhd5NigQ>? M13sdFEhcHJ? NUPsSXVDUW6qaXLpeIlwdiCxZjDETFEhWjF|MlOgcZV1[W62IHjvcY9lcW2ncjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBU\jliY3XscJMheHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViYXTkbZRqd25ib3[gZYxxcGFvS1eg[o9tdG:5ZXSgZpkhPjBibXnud{BqdmO3YnH0bY9vKGmwIIDy[ZNmdmOnIH;mJG5CTFCKLDDORWRRNCCmaXHwbI9z[XOnIHHu[EBz\XOjeoXybY4h[nliZnz1c5Jme2OnbnPlJJNx\WO2cn;t[ZRzgSxiSVO1NFwxNjB3zszN NH3jVZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1Ojd7MES3M{c,S2iHTVLMQE9iRg>?
Sf9 NWnlOYRJTnWwY4Tpc44h[XO|YYm= MXuxJIhz NHSzZ5pKdmirYnn0bY9vKG:oIFnETFIhWjF2MGGgcZV1[W62IHjvcY9lcW2ncjCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBU\jliY3XscJMheHKnLXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViYXTkbZRqd25ib3[gZYxxcGFvS1eg[o9tdG:5ZXSgZpkhOTZiaILzJIlv[3WkYYTpc44hcW5icILld4Vv[2Vib3[gUmFFWEhuIF7BSHAtKGSrYYDoc5Jie2ViYX7kJJJme2G8dYLpckBjgSCobIXvdoV{[2WwY3Wgd5Bm[3S{b33leJJ6KGKjc3XkJINw\mFuIFnDOVA9OC5yNd88US=> MlXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
HT1080 MkOySpVv[3Srb36gZZN{[Xl? M2\5OlQ5KGi{cx?= Ml\ETY5pcWKrdHnvckBw\iCLRFixJHIyOzKKL2KxN|JEKG23dHHueEBqdiCqdX3hckBJXDFyOECgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKDJvSFeg[o9zdWG2aX;uJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IFzDMW1UKG2ndHjv[EwhUUN3MEywMlA2|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
U87MG M3zHSGZ2dmO2aX;uJIF{e2G7 NUDBZ5ZSPDhiaILz NYTremxrUW6qaXLpeIlwdiCxZjDJSGgyKFJzM{LDJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBpfW2jbjDVPFdOTyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gNk1JTyCob4LtZZRqd25iaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVENvTWOgcYV1cG:mLDDJR|UxRDBwMEZOwG0> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0Nlc6ODR5Lze+R4hGVUKOPD;hQi=>
TS603 NIL2WmxHfW6ldHnvckBie3OjeR?= MWG0PEBpenN? MkHTTY5pcWKrdHnvckBw\iCGSEGgVlE{OkhibYX0ZY51KGmwIHj1cYFvKFSVNkCzJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiB{LVjHJIZwem2jdHnvckBqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDMR{1OWyCvZYToc4QtKEmFNUC8NE4xPc7:TR?= Mm[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFI4QTB2Nz:nQmNpTU2ETEyvZV4>
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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Molarity Calculator

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Clinical Trial Information

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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