2. Metabolic Enzyme/Protease Apoptosis
  3. Oxidative Phosphorylation Mitochondrial Metabolism Apoptosis
  4. IACS-010759 hydrochloride

IACS-010759 hydrochloride  (Synonyms: IACS-10759 hydrochloride)

Cat. No.: HY-112037A Purity: 99.82%
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IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research.

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

IACS-010759 hydrochloride Chemical Structure

IACS-010759 hydrochloride Chemical Structure

CAS No. : 1807523-99-4

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 220 In-stock
25 mg USD 450 In-stock
50 mg USD 650 In-stock
100 mg USD 950 In-stock
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500 mg   Get quote  

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Based on 10 publication(s) in Google Scholar

Other Forms of IACS-010759 hydrochloride:

IACS-010759 hydrochloride Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research[1][2].

IC50 & Target

OXPHOS[1]
In Vitro

IACS-010759 hydrochloride (10, 30, 100?nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML[1].
? IACS-010759 hydrochloride (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 hydrochlorideis similarly active in mouse (average IC50?=?5.6?nM), rat (IC50?=?12.2?nM), and cynomolgus monkey (IC50?=?8.7?nM) cell lines[1].
?

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

IACS-010759 hydrochloride Related Antibodies
In Vivo

IACS-010759 hydrochloride (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 hydrochloride (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

599.02

Formula

C25H26ClF3N6O4S
CAS No.
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.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 60 mg/mL (100.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6694 mL 8.3470 mL 16.6939 mL
5 mM 0.3339 mL 1.6694 mL 3.3388 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.82%

COA (248 KB) HNMR (302 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6694 mL 8.3470 mL 16.6939 mL 41.7348 mL
5 mM 0.3339 mL 1.6694 mL 3.3388 mL 8.3470 mL
10 mM 0.1669 mL 0.8347 mL 1.6694 mL 4.1735 mL
15 mM 0.1113 mL 0.5565 mL 1.1129 mL 2.7823 mL
20 mM 0.0835 mL 0.4173 mL 0.8347 mL 2.0867 mL
25 mM 0.0668 mL 0.3339 mL 0.6678 mL 1.6694 mL
30 mM 0.0556 mL 0.2782 mL 0.5565 mL 1.3912 mL
40 mM 0.0417 mL 0.2087 mL 0.4173 mL 1.0434 mL
50 mM 0.0334 mL 0.1669 mL 0.3339 mL 0.8347 mL
60 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.6956 mL
80 mM 0.0209 mL 0.1043 mL 0.2087 mL 0.5217 mL
100 mM 0.0167 mL 0.0835 mL 0.1669 mL 0.4173 mL
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IACS-010759 hydrochloride 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.

Keywords:

IACS-0107591807523-99-4IACS-10759IACS010759IACS 010759IACS10759IACS 10759Oxidative PhosphorylationMitochondrial MetabolismApoptosisorallymitochondrialcomplexIoxidativephosphorylationOXPHOSAMLH460Inhibitorinhibitorinhibit

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