Ivosidenib
Ivosidenib Basic information
- Product Name:
- Ivosidenib
- Synonyms:
-
- AG120;AG 120
- RG120
- Ivosidenib
- CS-1721
- lvosidenib
- RG120 100MG
- EOS-60845
- Ivosidenib(AG-120)
- CAS:
- 1448347-49-6
- MF:
- C28H22ClF3N6O3
- MW:
- 582.96
- Product Categories:
-
- API
- Mol File:
- 1448347-49-6.mol
Ivosidenib Chemical Properties
- 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)
- pka
- 11.58±0.40(Predicted)
- form
- Solid
- color
- White to Off-White
Ivosidenib Usage And Synthesis
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. AG-120 may induce cellular differentiation as well as inhibit proliferation in IDH1-expressing tumor cells.
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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