Enasidenib, Free Base

Enasidenib, Free Base
Item number Size Datasheet Manual SDS Delivery time Quantity Price
LC-E-2121_5mg 5 mg -

3 - 15 business days*

72.00€
LC-E-2121_10mg 10 mg -

3 - 15 business days*

87.00€
LC-E-2121_25mg 25 mg -

3 - 15 business days*

93.00€
LC-E-2121_50mg 50 mg -

3 - 15 business days*

117.00€
LC-E-2121_100mg 100 mg -

3 - 15 business days*

189.00€
LC-E-2121_200mg 200 mg -

3 - 15 business days*

307.00€
LC-E-2121_500mg 500 mg -

3 - 15 business days*

615.00€
LC-E-2121_1g 1 g -

3 - 15 business days*

1,058.00€
LC-E-2121_2g 2 g -

3 - 15 business days*

1,620.00€
 
Soluble in DMSO. Enasidenib, also known as AG221, is a potent and selective IDH2 mutant enzyme... more
Product information "Enasidenib, Free Base"
Soluble in DMSO. Enasidenib, also known as AG221, is a potent and selective IDH2 mutant enzyme inhibitor. It caused a significant decrease in R(-)-2-hydroxyglutarate in marrow, plasma, and urine and showed a dose-dependent survival benefit in a primary human AML xenograft model carrying the IDH2 R140Q mutation. Wang F., et al. 'AG-221 Offers a Survival Advantage In a Primary Human IDH2 Mutant AML Xenograft Model.' Blood 122: Abstract 240 (2013). Enasidenib is an orally available selective potent inhibitor of the mutant IDH2 enzyme. It inhibited 2HG production by the IDH2R140Q homodimer (IC50 = 100 nM), the IDH2R140Q/WT heterodimer (IC50 = 30 nM), and the IDH2R172K/WT heterodimer (IC50 = 10 nM), and inhibited the canonical forward (oxidative) reaction in the IDH2WT homodimer (IC50 = 1.8 µM). It inhibited 2HG production and promoted cellular differentiation in primary human IDH2 mutation-positive acute myeloid leukemia (AML) cells ex vivo and in xenograft mouse models. It also provided significant survival benefit in an aggressive IDH2R140Q-mutant AML xenograft mouse model. Yen K., et al. 'AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations.' Cancer Discov. 7: 478-493 (2017). Differentiation appears to be the main mechanism of enasidenib efficacy in relapsed/refractory AML patients. Amatangelo M.D., et al. 'Enasidenib induces acute myeloid leukemia cell differentiation to promote clinical response.' Blood 130: 732-741 (2017).
Keywords: AG221
Supplier: LC Laboratories
Supplier-Nr: E-2121

Properties

Application: Antineoplastic, Potent, selective IDH2 mutant enzyme inhibitor
MW: 473.38 D
Formula: C19H17F6N7O
Purity: >99%
Format: Solid

Database Information

CAS : 1446502-11-9| Find alternatives
KEGG ID : K00031 | Find alternatives

Handling & Safety

Storage: -20°C
Shipping: +20°C (International: +20°C)
Signal Word: Warning
GHS Hazard Pictograms:
H Phrases: H302, H410
P Phrases: P264, P270, P273, P330, P391, P301+P312, P501
Caution
Our products are for laboratory research use only: Not for administration to humans!
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