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Technical Data
| Formula | C25H25F3N6O4S |
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| Molecular Weight | 562.56 | CAS No. | 1570496-34-2 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (177.75 mM) | |
| Water | Insoluble | |||
| Ethanol | 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 | IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I. | ||
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| In vitro | IACS-010759 significantly reduced viability measured by CTG assay in all cell lines tested (Notch mutant: Pf382, 1301, Jurkat, MOLT-4, P12-Ichikawa and Notch wt: T-ALL1). Treatment of T-ALL with IACS-010759 had effectively inhibited FA-stimulated mitochondrial respiration indicated by decreased oxygen consumption rates (OCR). However, the cells maintain an ability to generate energy via glycolysis, indicated by high extracellular acidification rate (ECAR) in both, control and IACS-treated groups[1]. In CLL cells, IACS-010759 causes minimal cell death, inhibits oxygen consumption rate (OCR) and increases glycolysis. It also decreases intracellular ribonucleotide triphosphate pools in CLL[2]. In sensitive AML cells IACS-010759 induces AMPK activation leading to mTOR suppression which results in cell growth inhibition in AML cells. AMPK and mTOR could be putative biomarkers of anti-leukemia activity of the novel OxPhosi IACS-010759[3]. |
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| In vivo | IACS-010759 is a potent inhibitor of mitochondria complex I of the electron transport chain. It inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on oxidative phosphorylation.[4] |
Protocol (from reference)
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References
Selleck's IACS-010759 (IACS-10759) has been cited by 39 publications
| Mitochondrial complex I promotes kidney cancer metastasis [ Nature, 2024, 10.1038/s41586-024-07812-3] | PubMed: 39143213 |
| Compensatory activity of the PC-ME1 metabolic axis underlies differential sensitivity to mitochondrial complex I inhibition [ Nat Commun, 2024, 15(1):8682] | PubMed: 39375345 |
| Self-renewing human naïve pluripotent stem cells dedifferentiate in 3D culture and form blastoids spontaneously [ Nat Commun, 2024, 15(1):668] | PubMed: 38253551 |
| Cyclin-dependent kinase 12 deficiency reprogrammes cellular metabolism to alleviate ferroptosis potential and promote the progression of castration-resistant prostate cancer [ Clin Transl Med, 2024, 14(5):e1678] | PubMed: 38736108 |
| Deoxycytidine kinase inactivation enhances gemcitabine resistance and sensitizes mitochondrial metabolism interference in pancreatic cancer [ Cell Death Dis, 2024, 15(2):131] | PubMed: 38346958 |
| Multivariate analysis of metabolic state vulnerabilities across diverse cancer contexts reveals synthetically lethal associations [ Cell Rep, 2024, 43(10):114775] | PubMed: 39305483 |
| Preneoplastic cells switch to Warburg metabolism from their inception exposing multiple vulnerabilities for targeted elimination [ Oncogenesis, 2024, 13(1):7] | PubMed: 38272902 |
| Characterizing OXPHOS inhibitor-mediated alleviation of hypoxia using high-throughput live cell-imaging [ Cancer Metab, 2024, 12(1):13] | PubMed: 38702787 |
| Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8] | PubMed: 38522556 |
| Targeting Asparagine Metabolism in Well-Differentiated/Dedifferentiated Liposarcoma [ Cancers (Basel), 2024, 16(17)3031] | PubMed: 39272889 |
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.