| Identification | Back Directory | [Name]
RG120 | [CAS]
1448347-49-6 | [Synonyms]
RG120
CS-1721
EOS-60845
lvosidenib
Ivosidenib
RG120 100MG
AG120;AG 120
AG-120 (RG120)
Ivosidenib 13C5
13C5]-Ivosidenib
Ivosidenib(AG-120)
(2S)-1-(4-Cyano-2-pyridinyl)-5-oxo-L-prolyl-2-(2-chlorophenyl)-N-(3,3-difluorocyclobutyl)-N2-(5-fluoro-3-pyridinyl)glycinamide
Glycinamide, 1-(4-cyano-2-pyridinyl)-5-oxo-L-prolyl-2-(2-chlorophenyl)-N-(3,3-difluorocyclobutyl)-N2-(5-fluoro-3-pyridinyl)-, (2S)-
(S)-N-[(S)-1-(2-Chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl]-1-(4-cyano-2-pyridyl)-N-(5-fluoro-3-pyridyl)-5-oxopyrrolidine-2-carboxamide
(S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
(2S)-N-{(1S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl}-1(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide | [Molecular Formula]
C28H22ClF3N6O3 | [MDL Number]
MFCD29036964 | [MOL File]
1448347-49-6.mol | [Molecular Weight]
582.96 |
| Chemical Properties | Back Directory | [Melting point ]
151-173°C | [Boiling point ]
854.3±65.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer, Under inert atmosphere | [solubility ]
Chloroform (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
11.58±0.40(Predicted) | [color ]
White to Off-White | [InChIKey]
KZEDTWHGUDPGAF-UPVQGACJSA-N | [SMILES]
C(N(C1N(O)CC=C(C#N)C=1)C(=O)[C@@H]1CCON1)(=O)[C@H](C1=CC=CC=C1Cl)N(C1CC(F)(F)C1)C1=CC(F)=CN=C1 |
| Hazard Information | Back Directory | [Description]
AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) that specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of 2-hydroxyglutarate.1 AG-120 may induce cellular differentiation as well as inhibit proliferation in IDH1-expressing tumor cells.1 | [Uses]
Ivosidenib is a first-in-class mutant IDH1 inhibitor for the treatment of IDH1 mutant cancers. | [Definition]
ChEBI: Ivosidenib is a tertiary carboxamide resulting from the formal condensation of the carboxy group of (2S)-1-(4-cyanopyridin-2-yl)-5-oxopyrrolidine-2-carboxylic acid with the secondary amino group of (2S)-2-(2-chlorophenyl)-N-(3,3-difluorocyclobutyl)-2-[(5-fluoropyridin-3-yl)amino]acetamide. It is approved by the FDA for the treatment of acute myeloid leukemia (AML) in patients with an isocitrate dehydrogenase-1 (IDH1) mutation. It has a role as an antineoplastic agent and an EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor. It is a member of monochlorobenzenes, a cyanopyridine, a member of pyrrolidin-2-ones, an organofluorine compound, a tertiary carboxamide and a secondary carboxamide. | [in vitro]
tf-1 cells or primary human aml patient samples expressing mutant idh1 were treated with ag-120, and the results showed that in tf-1 idh1-r132h cells, ag-120 was able to decrease the intracellular 2-hg levels, inhibit growth factor independent proliferation and restore erythropoietin-induced differentiation [1]. | [IC 50]
< 100 nm | [storage]
Store at -20°C | [References]
[1] erica hansen et al. ag-120, an oral, selective, first-in-class, potent inhibitor of mutant idh1, reduces intracellular 2hg and induces cellular differentiation in tf-1 r132h cells and primary human idh1 mutant aml patient samples treated ex vivo. blood 2014 124:3734.
[2] http://www. aacr.org/newsroom/pages/news-release-detail.aspx itemid=789#.wlauom997iu |
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