2. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Lipoxygenase Apoptosis Reactive Oxygen Species (ROS) FAK
  4. LXG6403

LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors.

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LXG6403

LXG6403 Chemical Structure

CAS No. : 315705-04-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

LXG6403 Related Antibodies

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Description

LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors[1].

In Vitro

LXG6403 (Compound 9) inhibits the cellular LOX activity with IC50s of 1.3 μM (MDA-MB-231 cells), 1.43 μM (HCC143 cells), 4.14 μM (Hs-578-T cells), and 3.0 μM (HCC1937 cellss)[1].

LXG6403 (0-10 μM) inhibits rLOX, rLOXL2, rLOX-CM, rLOXL2-CM activity ,with IC50s of 0.28 μM, 0.95 μM, 0.95 μM, 2.82 μM respectively, does not inhibit rLOXL1 (IC50 > 10 μM) in HEK293T cells[1].

LXG6403 (0-20 μM) inhibits pronase-mediated degradation of LOX[1].

LXG6403 (15 μM, 48 h) enhances response to the anthracycline, Doxorubicin (HY-15142A); the platinum-based agent, Cisplatin (HY-17394); and the taxane, Paclitaxel (HY-B0015) in the TNBC cells, MDA-MB-231, and HCC1143 in 3D collagen I[1].

LXG6403 (9 days) reduces organoid viability and size with chemotherapeutic agents; Doxorubicin, Cisplatin, or Paclitaxel[1].

LXG6403 (20 µM, 48 h) inhibits the migration capacity of the highly migratory MDA-MB-231 cells[1].

LXG6403 (15 μM) reduces deposition of collagen and fibronectin within the ECM and inhibited their assembly[1].

LXG6403 improves Doxorubicin penetration in 3D collagen I-embedded TNBC cell lines and PDX organoids[1].

LXG6403 inhibits LOX, increases drug penetration in 3D culture, induces ROS generation/DNA damage and inhibits FAK signaling, leading to G1 arrest and apoptosis in TNBC cell lines and organoids in MDA-MB-231 cells[1].

LXG6403 (2.5-20 μM) not change cell viability in MCF12A, HUVEC, and HFF-1 cells[1].

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

LXG6403 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 20 μM
Incubation Time: 24 h, 48 h
Result: Increased γ-H2AX levels, cleaved caspase-3 and cleaved PARP levels, and decreased FAK phosphorylation.
Parmacokinetics
Species Dose Route CL T1/2 Cmax AUC Vd Vd/F
Mice 25 mg/kg p.o. 7.1 mL/min/kg 4.6 h 14.8 μg/mL 60.8 μg·h/mL 2.8 L/kg /
Mice 50 mg/kg p.o. 9.4 mL/min/kg 4.4 h 19.8 μg/mL 88.9 μg·h/mL / 3.6 L/kg
In Vivo

LXG6403 (Compound 9) (25-200 mg/kg, p.o., 5 days) does not change body weight or blood cell counts and does not cause organ damage in BALB/c mice[1].

LXG6403 (50 mg/kg, p.o., daily, 24 days) reduces fibrillar collagen content/crosslinking, leading to increased drug penetration and ROS accumulation, inhibits FAK signaling, induces DNA damage, G1 arrest, and apoptosis combined with Doxorubicin treatment in the resistant TM01278 TNBC PDX mice model with high LOX expression[1].

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

Animal Model: TM01278 TNBC PDX mice model[1]
Dosage: 50 mg/kg
Administration: p.o., daily, 24 days
Result: Reduced tumor growth and tumor weight without changing body weight combined with Doxorubicin.
Reduced fibrillar collagen and insoluble collagen content combined with Doxorubicin.
Increased doxorubicin penetration in vivo, increased ROS accumulation (and DNA damage, further leading to FAK inhibition, induction of G1 arrest and apoptosis combined with Doxorubicin.
Molecular Weight

345.44

Formula

C15H15N5OS2
CAS No.
Appearance

Solid

Color

Off-white to pale purple

SMILES

O=C(C)NC1=CC=C(NC2=NC(C3=C(C)N=C(N)S3)=CS2)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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (289.49 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 2.8949 mL 14.4743 mL 28.9486 mL
5 mM 0.5790 mL 2.8949 mL 5.7897 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 3.75 mg/mL (10.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.75 mg/mL (10.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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
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. 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 2.8949 mL 14.4743 mL 28.9486 mL 72.3715 mL
5 mM 0.5790 mL 2.8949 mL 5.7897 mL 14.4743 mL
10 mM 0.2895 mL 1.4474 mL 2.8949 mL 7.2371 mL
15 mM 0.1930 mL 0.9650 mL 1.9299 mL 4.8248 mL
20 mM 0.1447 mL 0.7237 mL 1.4474 mL 3.6186 mL
25 mM 0.1158 mL 0.5790 mL 1.1579 mL 2.8949 mL
30 mM 0.0965 mL 0.4825 mL 0.9650 mL 2.4124 mL
40 mM 0.0724 mL 0.3619 mL 0.7237 mL 1.8093 mL
50 mM 0.0579 mL 0.2895 mL 0.5790 mL 1.4474 mL
60 mM 0.0482 mL 0.2412 mL 0.4825 mL 1.2062 mL
80 mM 0.0362 mL 0.1809 mL 0.3619 mL 0.9046 mL
100 mM 0.0289 mL 0.1447 mL 0.2895 mL 0.7237 mL
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  • 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:

LXG6403315705-04-5LXG 6403LXG-6403LipoxygenaseApoptosisReactive Oxygen Species (ROS)FAKLOXPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorMDA-MB-231 cellsHEK293T mammalian cellsTM01278 TNBC PDX modelinhibitorinhibit

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