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Technical Data
| Formula | C21 H18 F3 N3 O3 S2 |
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| Molecular Weight | 481.51 | CAS No. | 1432660-47-3 | |
| Solubility (25°C)* | In vitro | DMSO | 96 mg/mL (199.37 mM) | |
| Ethanol | 96 mg/mL (199.37 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. | ||
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| In vitro | AGI-6780 potently reduce (R)-2-hydroxyglutarate (2HG) levels in cell lines ectopically overexpressing IDH2/R140Q with EC50 of 20 nM, with excellent selectivity against other dehydrogenases. AGI-6780 reverses the IDH2/R140Q-induced differentiation block in TF-1 cells, and induces blast differentiation in primary human IDH2/R140Q AML patient samples. [1] |
Protocol (from reference)
Customer Product Validation
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Data from [Data independently produced by , , Blood, 2018, doi: 10.1182/blood-2018-05-850826]
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Data from [Data independently produced by , , Theranostics, 2018, 8(15):4050-4061]
Selleck's AGI-6780 has been cited by 13 publications
| Wild-type IDH2 is a therapeutic target for triple-negative breast cancer [ Nat Commun, 2024, 15(1):3445] | PubMed: 38658533 |
| Targeting PRMT1 prevents acute and chronic graft-versus-host disease [ Mol Ther, 2023, 10.1016/j.ymthe.2023.09.011] | PubMed: 37735873 |
| IDH2 stabilizes HIF-1α-induced metabolic reprogramming and promotes chemoresistance in urothelial cancer [ EMBO J, 2023, e110620.] | PubMed: 36637036 |
| Aberrant metabolite trafficking and fuel sensitivity in human pluripotent stem cell-derived islets [ Cell Rep, 2023, 42(8):112970] | PubMed: 37556323 |
| Targeting Mitochondrial IDH2 Enhances Antitumor Activity of Cisplatin in Lung Cancer via ROS-Mediated Mechanism [ Biomedicines, 2023, 11(2)475] | PubMed: 36831011 |
| Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] | PubMed: 35868306 |
| Reductive TCA cycle catalyzed by wild-type IDH2 promotes acute myeloid leukemia and is a metabolic vulnerability for potential targeted therapy [ J Hematol Oncol, 2022, 15(1):30] | PubMed: 35313945 |
| Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182] | PubMed: 36248745 |
| Mitofusin2 Promotes β Cell Maturation from Mouse Embryonic Stem Cells via Sirt3/Idh2 Activation [ Stem Cells Int, 2022, 2022:1172795] | PubMed: 35386849 |
| Wild-type IDH2 protects nuclear DNA from oxidative damage and is a potential therapeutic target in colorectal cancer [ Oncogene, 2021, 10.1038/s41388-021-01968-2] | PubMed: 34349242 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.