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IACS-010759

Catalog No. T5337   CAS 1570496-34-2
Synonyms: IACS-10759, IACS 10759, IACS10759

IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
IACS-010759 Chemical Structure
IACS-010759, CAS 1570496-34-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 47.00
2 mg In stock $ 67.00
5 mg In stock $ 115.00
10 mg In stock $ 177.00
25 mg In stock $ 372.00
50 mg In stock $ 538.00
100 mg In stock $ 788.00
200 mg In stock $ 1,070.00
1 mL * 10 mM (in DMSO) In stock $ 152.00
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Purity: 99.83%
Purity: 99.73%
Purity: 98.18%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.
In vitro Treatment of primary CLL cells with IACS-010759 greatly inhibited oxidative phosphorylation (OxPhos) but caused only minor cell death at 24 and 48 h [1]. KPS-tumor-derived murine cells were more sensitive to IACS-010759 compared to KP-tumor-derived cell lines [2]. Established AML cell lines were exposed to a range of IACS-010759 concentrations for 3–7 d, resulting in reduced viability with EC50 values of<3nM [3].
In vivo In mice following intravenous (0.3mg per kg body weight (mg/kg)) and oral (1mg/kg) administration, IACS-010759 was characterized by low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24h) of IACS-010759 with sustained levels of compound in the plasma following oral dosing. Treatment with IACS-010759 at the 5 or 10mg/kg dose resulted in tumor regression with minimal body weight loss, whereas IACS-010759 at the 25mg/kg dose was not tolerated, and body weight loss, lethargy, and hypothermia were observed [3].
Cell Research CLL cells were incubated with either dimethyl sulfoxide (control) or IACS-010759 (100 nM) for 24 h. A total of 10^6 cells were stained with MitoSOX Red and tetramethylrhodamine ethyl ester perchlorate and were analyzed using flow cytometry for mitochondrial reactive oxygen species (ROS) and mitochondrial outer membrane potential, respectively [1].
Animal Research OCI-AML3 cells were expanded in RPMI medium + 5% or 10% fetal bovine serum (FBS) until ≥150 million cells were present. For OCI-AML3, 2 million cells in 200 μl of saline were injection into the tail vein of NSG mice. For the patient-derived models, 4030094 and S6-AP, cells were harvested from mice with advanced disease or resuscitated from frozen vials, washed and resuspended at 5 x 10^6 cells/ml in PBS. Mice were irradiated for 24 hours at 250 cGY before orthotopic implantation of 1 x 10^6 cells suspended in 200 μl of saline were into the tail vein of 6- to 8-week old female NSG mice. For OCI-AML3, treatment began when whole body luminescence averaged 5 x 10^7. For model 4030094, treatment for the efficacy began when animals reached 10% burden and for the PK/PD studies when the animals reached 80% disease burden as measured by human and mouse CD45 and viability (DAPI 62248) staining followed by flow cytometry with a Fortessa flow cytometer. Mice were randomized based on luminescence for the OCI-AML3 model and by disease burden (hCD45+) for the patient-derived xenograft. Cohorts of mice were sacrificed 21 days after study drug initiation to collect spleen and bone marrow or followed for overall survival while continuing study drug [3].
Synonyms IACS-10759, IACS 10759, IACS10759
Molecular Weight 562.56
Formula C25H25F3N6O4S
CAS No. 1570496-34-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (53.3 mM)

TargetMolReferences and Literature

1. Vangapandu HV, et al. Biological and metabolic effects of IACS-2010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells. Oncotarget. 2018 May 18;9(38):24980-241991. 2. Lissanu Deribe Y, et al. Mutations in the SWI/SNF complex induce a targetable dependence on oxidative phosphorylation in lung cancer. Nat Med. 2018 Jul;24(7):1047-1057. 3. Molina JR, et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046.

TargetMolCitations

1. Ren L, Meng L, Gao J, et al.PHB2 promotes colorectal cancer cell proliferation and tumorigenesis through NDUFS1-mediated oxidative phosphorylation.Cell Death & Disease.2023, 14(1): 44. 2. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023 3. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Active Compound Library Mitochondria-Targeted Compound Library Anti-Cancer Compound Library Bioactive Compound Library Apoptosis Compound Library Drug Repurposing Compound Library Inhibitor Library

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Keywords

IACS-010759 1570496-34-2 Apoptosis Metabolism Others Mitochondrial Metabolism OXPHOS phosphorylation complex mitochondrial IACS-10759 Inhibitor orally IACS 010759 inhibit H460 AML IACS010759 IACS 10759 IACS10759 oxidative inhibitor

 

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