Enasidenib
- Product Name
- Enasidenib
- CAS No.
- 1446502-11-9
- Chemical Name
- Enasidenib
- Synonyms
- NameC;AG-211;AG-221;CS-1590;CC90007;CC 90007;CC-90007;Enasidenib;AG221;AG 221;Enasidenib(AG-221)
- CBNumber
- CB53044318
- Molecular Formula
- C19H17F6N7O
- Formula Weight
- 473.38
- MOL File
- 1446502-11-9.mol
Enasidenib Property
- Melting point:
- 168-170°C
- Boiling point:
- 581.0±60.0 °C(Predicted)
- Density
- 1.477±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (up to 25 mg/ml)
- form
- solid
- pka
- 14.70±0.29(Predicted)
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 21277
- Product name
- Enasidenib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $97
- Updated
- 2024/03/01
- Product number
- 21277
- Product name
- Enasidenib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
- Product number
- 21277
- Product name
- Enasidenib
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $433
- Updated
- 2024/03/01
- Product number
- 21277
- Product name
- Enasidenib
- Purity
- ≥98%
- Packaging
- 100mg
- Price
- $1151
- Updated
- 2024/03/01
- Product number
- 474054
- Product name
- AG 221
- Packaging
- 100mg
- Price
- $1296
- Updated
- 2021/12/16
Enasidenib Chemical Properties,Usage,Production
Description
Enasidenib (1446502-11-9) is a potent (IC50’s = 100 nM IDH2R140Q homodimer, 30 nM IDH2R140Q/WT heterodimer and 10 nM IDH2R172K/WT heterodimer) and selective inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).1? It suppressed the production of the oncometabolite (R)-2-Hydroxyglutarate (a competitive inhibitor of αKG-dependent dioxygenases which leads to epigenetic dysregulation) and induced cellular differentiation in primary human IDH2 mutation-positive acute myeloid leukemia cells.1,2? Recently approved for clinical use by the FDA.
Uses
Enasidenib is a first-in-class oral selective inhibitor of mutant IDH2 enzymes (isocitrate dehydrogenase 2), for the treatment of adults with relapsed or refractory IDH2-mutated acute myeloid leukemia.
Definition
ChEBI: Enasidenib is a 1,3,5-triazine which is substituted by (2-hydroxy-2-methylpropyl)nitrilo, 6-(trifluoromethyl)pyridin-2-yl and [2-(trifluoromethyl)pyridin-4-yl]nitrilo groups at positions 2,4 and 6, respectively. It is an isocitrate dehydrogenase-2 (IDH2) inhibitor which has been approved for the treatment of adults with relapsed or refractory acute myeloid leukaemia (AML). It has a role as an antineoplastic agent and an EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor. It is an aminopyridine, an organofluorine compound, a secondary amino compound, a tertiary alcohol, a member of 1,3,5-triazines and an aromatic amine.
in vitro
ag-221 was found to be able to reduce 2-hg levels by >90%, reverse in-vitro histone and dna hypermethylation, and induce differentiation in leukemia cell model as well. in addition, a dose dependent proliferative burst of the human specific cd45+ blast cells was observed by the treatment of ag-221, as measured by the expression of cd11b, cd14, cd15 and cell morphology [1].
in vivo
the efficacy of ag-221 in a primary human aml xenograft model with the idh2 r140q mutation was studied, and the results showed that ag-221 could reduce 2-hg in the plasma, bone marrow, and urine of engrafted mice potently. in addition, the treatment of ag-221 could also induce a significant and dose dependent survival benefit as demonstrated by that all mice in the high dose treatment of ag-221 survived to the end of study [1].
IC 50
~16 nm for idh2 r140q mutant
References
1) Yen et al. (2017), AG-221, A First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations; Cancer Discov. 7 478 2) Amatangelo et al. (2017), Enasidenib induces acute myeloid leukemia cell differentiation to promote clinical response; Blood 130 732
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