Enasidenib

Enasidenib Suppliers list
Company Name: ATK CHEMICAL COMPANY LIMITED
Tel: +undefined-21-51877795
Email: ivan@atkchemical.com
Products Intro: CAS:1446502-11-9
Purity:98% Package:10MG;50MG;100MG,1G,5G,10G.100G
Company Name: BOC Sciences
Tel: +1-631-485-4226
Email: inquiry@bocsci.com
Products Intro: Product Name:Enasidenib
CAS:1446502-11-9
Purity:98% Package:50mg Remarks:BOC Sciences also provides custom synthesis services for Enasidenib.
Company Name: SHANGHAI T&W PHARMACEUTICAL CO., LTD.
Tel: +86-021-61551413 +8618813727289
Email: contact@trustwe.com
Products Intro: Product Name:ag-221 Enasidenib
CAS:1446502-11-9
Purity:98% Package:Package as requetsed
Company Name: Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd
Tel: +86-86-22-87899925 +86-8618522618860
Email: 18522618860@163.com
Products Intro: Product Name:ag-221 Enasidenib
CAS:1446502-11-9
Purity:0.99 Package:Various Packaging; segregation
Company Name: TargetMol Chemicals Inc.
Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Products Intro: Product Name:Enasidenib;AG-221
CAS:1446502-11-9
Purity:99.45% Package:10 mg;100 mg;200 mg;5 mg;50 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
Enasidenib Basic information
Product Name:Enasidenib
Synonyms:Enasidenib(AG-221);AG-221 (Enasidenib);AG-211;2-Methyl-1-(4-(6-(trifluoromethyl)pyridin-2-yl)-6-(2-(trifluoromethyl)pyridin-4-ylamino)-1,3,5-triazin-2-ylamino)propan-2-ol;Enasidenib;AG-221;2-Propanol, 2-methyl-1-[[4-[6-(trifluoromethyl)-2-pyridinyl]-6-[[2-(trifluoromethyl)-4-pyridinyl]amino]-1,3,5-triazin-2-yl]amino]-;Enasidenib Mesylate
CAS:1446502-11-9
MF:C19H17F6N7O
MW:473.38
EINECS:
Product Categories:Inhibitors
Mol File:1446502-11-9.mol
Enasidenib Structure
Enasidenib Chemical Properties
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
pka14.70±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.
Safety Information
MSDS Information
Enasidenib Usage And Synthesis
DescriptionEnasidenib (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.
UsesEnasidenib 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.
DefinitionChEBI: 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 vitroag-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 vivothe 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
References1) 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
Enasidenib Preparation Products And Raw materials
Tag:Enasidenib(1446502-11-9) Related Product Information
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