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
- Molecular Weight:
- 473.38
- MDL Number:
- MFCD29472245
- MOL File:
- 1446502-11-9.mol
| 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. |
| NCI Dictionary of Cancer Terms | enasidenib mesylate |
| FDA UNII | 3T1SS4E7AG |
| NCI Drug Dictionary | enasidenib mesylate |
| ATC code | L01XX59 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P280-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Enasidenib price More Price(25)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 21277 | Enasidenib ≥98% | 1446502-11-9 | 5mg | $97 | 2024-03-01 | Buy |
| Cayman Chemical | 21277 | Enasidenib ≥98% | 1446502-11-9 | 10mg | $184 | 2024-03-01 | Buy |
| Cayman Chemical | 21277 | Enasidenib ≥98% | 1446502-11-9 | 25mg | $433 | 2024-03-01 | Buy |
| Cayman Chemical | 21277 | Enasidenib ≥98% | 1446502-11-9 | 100mg | $1151 | 2024-03-01 | Buy |
| Usbiological | 474054 | AG 221 | 1446502-11-9 | 100mg | $1296 | 2021-12-16 | Buy |
Enasidenib Chemical Properties,Uses,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
Enasidenib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5738 | 58 |
| Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd | +86-86-22-87899925 +86-8618522618860 | 18522618860@163.com | China | 694 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | eric@witopchemical.com | China | 23556 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Nanjing Doge Biomedical Technology Co., Ltd | +86-25-58227606 +86-15305155328 | sales@dogechemical.com | China | 4128 | 58 |
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