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Enasidenib [1446502-11-9]

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Référence NB-64-12737-100mg

Conditionnement : 100mg

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Enasidenib

(Synonyms: AG-221) Copy Product Info

Synonyms: AG-221

Catalog No. T2346 Copy Product Info

Purity: 99.96%

Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity.

Cas No. 1446502-11-9

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.96%

Color:White

Product Introduction

Bioactivity

Description	Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity.
Targets & IC50	IDH2 (R172K):400 nM, IDH2 (R140Q):100nM
In vitro	The compound has been demonstrated to reduce 2-HG levels by >90% and reverse histone and deoxyribonucleic acid (DNA) hypermethylation in vitro, and to induce differentiation in leukemia cell models[2].
In vivo	Enasidenib is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. Treatment also induced a dose dependent, statistically significant, survival benefit. A proliferative burst of the human specific CD45+ blast cells is followed by cellular differentiation as measured by the expression of CD11b, CD14 and CD15 and cell morphology after Enasidenib treatment[2]. Enasidenib treatment also restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression and reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Clinicalal trials combining IDH2 inhibitors with other targeted AML therapies are warranted in order to increase therapeutic efficacy[1].
Synonyms	AG-221
Kinase Assay	Untranslated region-mediated luciferase reporter expression: HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control.

Chemical Properties

Molecular Weight	473.38
Formula	C₁₉H₁₇F₆N₇O
Cas No.	1446502-11-9
Smiles	CC(C)(O)CNc1nc(Nc2ccnc(c2)C(F)(F)F)nc(n1)-c1cccc(n1)C(F)(F)F
Relative Density.	1.477 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 100 mg/mL (211.25 mM), Sonication is recommended.

DMSO: 245 mg/mL (517.55 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.56 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1125 mL	10.5623 mL	21.1247 mL	105.6234 mL
5 mM	0.4225 mL	2.1125 mL	4.2249 mL	21.1247 mL
10 mM	0.2112 mL	1.0562 mL	2.1125 mL	10.5623 mL
20 mM	0.1056 mL	0.5281 mL	1.0562 mL	5.2812 mL
50 mM	0.0422 mL	0.2112 mL	0.4225 mL	2.1125 mL
100 mM	0.0211 mL	0.1056 mL	0.2112 mL	1.0562 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

IsocitrateDehydrogenase(IDH)IsocitrateDehydrogenaseIsocitrate Dehydrogenase (IDH)Isocitrate DehydrogenaseInhibitorinhibitIDH2IDHEnasidenibAG221AG 221

Related Tags: Enasidenib chemical structure | Enasidenib in vivo | Enasidenib in vitro | Enasidenib formula | Enasidenib molecular weight