Cat. No.: HY-112037

IACS-010759

(Synonyms: IACS-10759)

28 Cited Publications

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Based on 28 publication(s) in Google Scholar

IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.

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Pureté: 99.68%
CAS No.: 1570496-34-2
Formule: C₂₅H₂₅F₃N₆O₄S
Masse moléculaire:562.56

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

IACS-010759 Chemical Structure

CAS No.: 1570496-34-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (28)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

OXPHOS^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	9.63 nM Compound: IACS-010759	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 37392582]
HL-60	EC₅₀	3 nM Compound: 29; IACS.010759	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36893622]
KG-1	EC₅₀	3 nM Compound: 29; IACS.010759	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36893622]
KG-1	IC₅₀	63.84 nM Compound: IACS-010759	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 37392582]
NCI-H460	IC₅₀	1.4 nM Compound: IACS-010759	Cytotoxicity against human NCI-H460 cells assessed as reduction in galactose-dependent cell viability incubated for 3 days by IncuCyte live-cell imaging assay Cytotoxicity against human NCI-H460 cells assessed as reduction in galactose-dependent cell viability incubated for 3 days by IncuCyte live-cell imaging assay	[PMID: 34982568]
NCI-H460	IC₅₀	1.4 nM Compound: 29; IACS.010759	Inhibition of mitochondrial respiration in human NCI-H460 cells assessed as oxygen consumption rate incubated for 1 hr by Seahorse XF24 extracellular flux analyzer Inhibition of mitochondrial respiration in human NCI-H460 cells assessed as oxygen consumption rate incubated for 1 hr by Seahorse XF24 extracellular flux analyzer	[PMID: 36893622]
NCM460	IC₅₀	>1000 nM Compound: IACS-010759	Antiproliferative activity against human NCM460 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human NCM460 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 37392582]
THP-1	EC₅₀	3 nM Compound: 29; IACS.010759	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36893622]

In Vitro

IACS-010759 (10, 30, 100 nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML^[1].
IACS-010759 (0.001, 0.01, 0.1, 1, 10, 100, 1000 nM; 72 hurs) robustly inhibits both OCR and galactose-dependent H460 cell viability and has nearly identical IC₅₀ values of 1.4 nM^[1].
IACS-010759 is similarly active in mouse (average IC₅₀ = 5.6 nM), rat (IC₅₀ = 12.2 nM), and cynomolgus monkey (IC50 = 8.7 nM) cell lines^[1].
IACS-010759 (0.01-10 μM) yieldes a maximal reduction of growth of > 50% in the majority of cancer cell lines (24 of 30 pancreatic (PDAC), 19 of 20 ovarian, 13 of 16 triple-negative breast (TNBC), 8 of 10 non-small-cell lung (NSCLC)) and a subset (11of 30 PDAC, 10 of 20 ovarian, 5 of 16 TNBC, 2 of 10 NSCLC) exhibited > 100% growth inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

IACS-010759 (5, 10, 25 mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10 mg/kg dose in mice bearing NB-1 (PGD-null) subcutaneous xenografts. IACS-010759 at the 25 mg/kg dose is not tolerated^[1].
IACS-010759 HCl (10 mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent^[1].
IACS-010759 (0.3 mg/kg for iv; 1 mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24 h)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1570496-34-2
Appearance Solid
Masse moléculaire 562.56
Formule C₂₅H₂₅F₃N₆O₄S
Color White to off-white
SMILES

FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCC(S(=O)(C)=O)CC5)=CC=C4)C(C)=N3)=N2)C=C1
Synonyms

IACS-10759
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (28)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayCell Imaging/Staining

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Journal Impact Factor

Nat Commun

Oxidative phosphorylation is a metabolic vulnerability of endocrine therapy and palbociclib resistant metastatic breast cancers. [Abstract]

2023 Jul 14;14(1):4221. PMID: 37452026

IACS-010759 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jul 14;14(1):4221. [Abstract]

Response of HBCx-124 to different doses of IACS-010759 (10-75 mg/kg; 5 days per week) and to Metformin P values were calculated with the Mann-Whitney test (two-tailed).

IACS-010759 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jul 14;14(1):4221. [Abstract]

Effect of IACS-010759 (0.01 nM-100 μM; 72 h) on in vitro models of ER+ breast cancer sensitive and resistant cells. Relative viability of MCF7 WT/LTED/ PalboR and of T47D WT/LTED derivatives cells.

IACS-010759 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jul 14;14(1):4221. [Abstract]

MCF7-LTED and PalboR cells were treated with 1 μM IACS for 72 h and ROS levels were measured using CellROX and DCFDA staining.
J Adv Res

Mitochondrial fatty acid oxidation as the target for blocking therapy-resistance and inhibiting tumor recurrence: The proof-of-principle model demonstrated for ovarian cancer cells. [Abstract]

2025 Mar 17:S2090-1232(25)00186-9. PMID: 40107354
Cell Discov

Lineage-coupled clonal capture identifies clonal evolution mechanisms and vulnerabilities of BRAFV600E inhibition resistance in melanoma. [Abstract]

2022 Oct 6;8(1):102. PMID: 36202798
Adv Sci (Weinh)

Amphiregulin and Epiregulin Confer Radioresistance in Esophageal Squamous Cell Carcinoma Through Oxidative Phosphorylation. [Abstract]

2025 Nov 9:e07524. PMID: 41208199

IACS-010759 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 9:e07524. [Abstract]

IACS-010759 (7.5 mg/kg; p.o. every other day) enhances irradiation efficacy for ESCC xenograft tumors.
Adv Sci (Weinh)

Enzalutamide Sensitizes Castration-Resistant Prostate Cancer to Copper-Mediated Cell Death. [Abstract]

2024 Jun 10:e2401396. PMID: 38859590

IACS-010759 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 10:e2401396. [Abstract]

Cell viability was measured for 22Rv1 and C4-2B cells after treatment with IACS-010759 (0.01-1000 nM) in the presence or absence of Enzalutamide for 5 days.
Cell Rep Med

Estrogen-related receptor alpha drives mitochondrial biogenesis and resistance to neoadjuvant chemoradiation in esophageal cancer. [Abstract]

2022 Nov 15;3(11):100802. PMID: 36334593
Cell Death Dis

Inhibition of mitochondrial complex I induces mitochondrial ferroptosis by regulating CoQH2 levels in cancer. [Abstract]

2025 Apr 5;16(1):254. PMID: 40185704
Cancer Lett

Acidosis overrides molecular heterogeneity to shape therapeutically targetable metabolic phenotypes in colon cancers. [Abstract]

2025 Feb 1:217512. PMID: 39900217
Cell Death Discov

Targeting metabolic vulnerabilities: REV-ERB agonist SR9009 potentiates sorafenib efficacy in liver cancer. [Abstract]

2026 Jan 19;12(1):86. PMID: 41554703
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086
Blood Adv

Targeting bone marrow mesenchymal stromal cells-derived IL-6 to overcome acute myeloid leukemia chemoresistance. [Abstract]

2025 Jul 16:bloodadvances.2024015496. PMID: 40668612
JCI Insight

Mitochondrial metabolic rewiring sensitizes mTORC1 inhibitor persister cells to cuproptosis. [Abstract]

2025 Nov 24;10(22):e187448. PMID: 41277553
JCI Insight

Metabolic pathways within cTfh subsets and glucose-dependent activation of cTfh17 in SLE and healthy individuals. [Abstract]

2025 Jul 22;10(14):e189858. PMID: 40693461
Cancer Metab

Unveiling the powerhouse: ASCL1-driven small cell lung cancer is characterized by higher numbers of mitochondria and enhanced oxidative phosphorylation. [Abstract]

2025 Mar 31;13(1):16. PMID: 40165271
Commun Biol

FGFR3 oncogenic activation drives oxidative metabolic reprogramming in bladder cancer: a systems metabolomics approach. [Abstract]

2026 May 23. PMID: 42177363
Commun Biol

Setd2 inactivation sensitizes lung adenocarcinoma to inhibitors of oxidative respiration and mTORC1 signaling. [Abstract]

2023 Mar 10;6(1):255. PMID: 36899051
Sci Rep

Targeting tumor metabolic flexibility enhances radiotherapeutic efficacy via mitochondrial complex I Inhibition in an intracranial S180 sarcoma mouse model. [Abstract]

2025 Nov 28. PMID: 41310084
J Pharmacol Exp Ther

Phenotypic pharmacology of novel Complex I inhibitors eliciting tissue repair concurrent to control of inflammation. [Abstract]

2025 Jul 15;392(9):103661. PMID: 40782522
Carcinogenesis

SMARCA4/BRG1 deficiency induces a targetable dependence on oxidative phosphorylation in clear cell renal cell carcinoma. [Abstract]

2025 Jan 24:bgaf002. PMID: 39851260
Biochem Biophys Res Commun

Lactic acidosis switches cancer cells from dependence on glycolysis to OXPHOS and renders them highly sensitive to OXPHOS inhibitors. [Abstract]

2023 Sep 3:671:46-57. PMID: 37295355
Biochem Biophys Res Commun

SWATH-MS proteomics of PANC-1 and MIA PaCa-2 pancreatic cancer cells allows identification of drug targets alternative to MEK and PI3K inhibition. [Abstract]

2021 May 7:552:23-29. PMID: 33740661
Mutat Res

Saikosaponin-d mediates FOXG1 to reverse docetaxel resistance in prostate cancer through oxidative phosphorylation. [Abstract]

2024 Jul 23:829:111875. PMID: 39098234
Res Sq

2026 Jun 15.
bioRxiv

2025 Oct 3.
bioRxiv

Tumor Genotype Dictates Mitochondrial and Immune Vulnerabilities in Liver Cancer. [Abstract]

2025 Sep 11:2025.09.10.675369. PMID: 40964275
University of Cambridge

2025.
bioRxiv

2024 Mar 21.
bioRxiv

2023 Dec 20.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (88.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7776 mL

8.8879 mL

17.7759 mL

5 mM

0.3555 mL

1.7776 mL

3.5552 mL

10 mM

0.1778 mL

0.8888 mL

1.7776 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (3.70 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Jennifer R Molina, et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046. [Content Brief]

[2]. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7776 mL	8.8879 mL	17.7759 mL	44.4397 mL
	5 mM	0.3555 mL	1.7776 mL	3.5552 mL	8.8879 mL
	10 mM	0.1778 mL	0.8888 mL	1.7776 mL	4.4440 mL
	15 mM	0.1185 mL	0.5925 mL	1.1851 mL	2.9626 mL
	20 mM	0.0889 mL	0.4444 mL	0.8888 mL	2.2220 mL
	25 mM	0.0711 mL	0.3555 mL	0.7110 mL	1.7776 mL
	30 mM	0.0593 mL	0.2963 mL	0.5925 mL	1.4813 mL
	40 mM	0.0444 mL	0.2222 mL	0.4444 mL	1.1110 mL
	50 mM	0.0356 mL	0.1778 mL	0.3555 mL	0.8888 mL
	60 mM	0.0296 mL	0.1481 mL	0.2963 mL	0.7407 mL
	80 mM	0.0222 mL	0.1111 mL	0.2222 mL	0.5555 mL

IACS-010759

28 Cited Publications

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IACS-010759

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Cuproptosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) IACS-010759

Activité biologique

Chemical Information

Publications (28)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

IACS-010759 Related Classifications

HY-112037 Related Classifications