LXG6403
Based on 1 Customer Validation
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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- Purity: 99.85%
- CAS No.: 315705-04-5
- 화학식: C15H15N5OS2
- 분자량:345.44
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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Metabolism/Protease Compound Library
HY-L012
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NF-κB Signaling Compound Library
HY-L014
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Ferroptosis Compound Library
HY-L051
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Cytoskeleton Compound Library
HY-L060
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Orally Active Compound Library
HY-L061
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Lipid Metabolism Compound Library
HY-L091
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Anti-Pulmonary Fibrosis Compound Library
HY-L125
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Coagulation and Anti-coagulation Compound Library
HY-L136
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Drug-Resistant Compound Library
HY-L169
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Fibrosis Compound Library
HY-L185
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Biological Activity
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.
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Cell Line:MDA-MB-231 cells
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Concentration:20 μM
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Incubation Time:24 h, 48 h
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Result:Increased γ-H2AX levels, cleaved caspase-3 and cleaved PARP levels, and decreased FAK phosphorylation.
| 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 |
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.
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Animal Model:TM01278 TNBC PDX mice model[1]
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Dosage:50 mg/kg
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Administration:p.o., daily, 24 days
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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.
Chemical Information
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CAS No. 315705-04-5
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Appearance Solid
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분자량 345.44
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화학식 C15H15N5OS2
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Color Off-white to pale purple
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SMILES
O=C(C)NC1=CC=C(NC2=NC(C3=C(C)N=C(N)S3)=CS2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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. 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 |
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| 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 |
LXG6403 Related Classifications
HY-171955 Related Classifications
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