IACS-010759 (Synonyms: IACS-10759)

Name: IACS-010759
Brand: MedChemExpress
SKU: HY-112037
Rating: 5.0 (26 reviews)

Cat. No.: HY-112037 Purity: 99.68%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 1570496-34-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of IACS-010759:

IACS-010759 hydrochloride In-stock

26 Publications Citing Use of MCE IACS-010759

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

Cell Imaging/Staining

: 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.

: 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.

: 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.

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Biological Activity
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References
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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: 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]
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]
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.

Clinical Trial

Molecular Weight

562.56

Formula

C₂₅H₂₅F₃N₆O₄S

CAS No.

1570496-34-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (247 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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

Complete Stock Solution Preparation Table

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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IACS-010759 (Synonyms: IACS-10759)

Customer Review

Other Forms of IACS-010759:

IACS-010759 Related Antibodies

26 Publications Citing Use of MCE IACS-010759

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•Related Screening Libraries:

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Biological Activity

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References

Customer Review

IACS-010759 Related Antibodies

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Complete Stock Solution Preparation Table

IACS-010759 Related Classifications

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