XEN445
Based on 1 publication(s) in Google Scholar
XEN445 is a potent, selective and orally active endothelial lipase (EL) inhibitor with an IC50 value of 0.237 μM. XEN445 selectively inhibits phospholipase enzymatic activity of LIPG. XEN445 raises plasma HDL and cholesterol levles. XEN445 induces G1 cell cycle arrest, reduces cell viability, suppresses cancer stem cell self-renewal, and inhibits tumor formation in LIPG-expressing triple-negative breast cancer cells, while showing no inhibitory effect on invasiveness or cancer stem cell stemness in these cells. XEN445 can be used for the research of cancer and metabolic disease, such as triple-negative breast cancer.
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- Purity: 99.63%
- CAS No.: 1515856-92-4
- 화학식: C18H17F3N2O3
- 분자량:366.33
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Publications Citing Use of MedChemExpress (MCE) XEN445
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.25 μM
Compound: 13, XEN445
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Inhibition of full length human endothelial lipase transfected in HEK293 cells using PED-A1 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
Inhibition of full length human endothelial lipase transfected in HEK293 cells using PED-A1 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
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[PMID: 24211162] |
XEN445 potently inhibits recombinant human endothelial lipase with an IC50 of 0.237 μM, and shows selectivity over human lipoprotein lipase ( IC50 = 20 μM) and human hepatic lipase ( IC50 = 9.5 μM)[1].
XEN445 (2.5 μM; 4 h) exhibits high binding to rat, mouse, and human plasma proteins, with 97.4%, 88.8%, and 95.4% binding respectively at 2.5 μM after 4 h at 37°C[1].
XEN445 potently inhibits recombinant human endothelial lipase-mediated hydrolysis of purified human HDL particles with an IC50 of 0.11 μM[1].
XEN445 (30 min) inhibits endothelial lipase activity in EL-transfected HEK-293 cells with an IC50 of 0.25 μM[1].
XEN445 (30 min) specifically inhibits LIPG phospholipase activity in parental and LIPG-overexpressing MDA-MB-468 cells, with an IC50 of 2.172 μM[2].
XEN445 (100-250 μM; 4 days) reduces viability of LIPG-expressing TNBC cells (MCF10DCIS, MDA-MB-468) via G1 cell cycle arrest in a LIPG-dependent manner[2].
XEN445 (250 μM; 3-4 days) enhances migration and invasion of LIPG-expressing TNBC cells (MDA-MB-468, MCF10DCIS)[2].
XEN445 (1 week) suppresses CSC self-renewal in LIPG-expressing TNBC cells (MCF10DCIS, MDA-MB-468)[2].
XEN445 upregulates expression of select stemness and EMT-related genes in LIPG-expressing TNBC cells (MDA-MB-468, MCF10DCIS)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF10DCIS, MDA-MB-468, MCF7, T47D, LIPG-overexpressing MDA-MB-468, LIPG-knockdown MDA-MB-468, LIPG-overexpressing MCF7 cells
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Concentration:1, 2.5, 5, 10, 25, 50, 100, 200, 250 μM
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Incubation Time:4 days
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Result:Reduced viability of MCF10DCIS cells at ≥100 μM.
Selectively reduced viability of LIPG-expressing TNBC cell lines (MCF10DCIS, MDA-MB-468) but not LIPG-negative luminal breast cancer cell lines (MCF7, T47D) at 200 and 250 μM.
Sensitized MDA-MB-468 and MCF7 cells to viability reduction via LIPG overexpression.
Rendered MDA-MB-468 cells resistant to viability reduction via LIPG knockdown.
XEN445 (50 mg/kg; i.p.; three times per week; 32 days) significantly inhibits in vivo triple-negative breast cancer xenograft tumor growth in nude mice were trans-
planted with MDA-MB-468 cells [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 12-16 weeks of age, wild-type)[1]
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Dosage:30 mg/kg
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Administration:p.o.; b.i.d.; 3 or 9 days
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Result:Increased total plasma cholesterol by 18% (from 106.1 mg/dL to 125.2 mg/dL) at 30 mg/kg for 3 days.
Increased plasma HDLc by 16% (from 74.7 mg/dL to 86.5 mg/dL) at 30 mg/kg for 3 days.
Increased total plasma cholesterol by 21% (from 108.3 mg/dL to 131.2 mg/dL) for 9 days.
Increased plasma HDLc by 30% (from 68.2 mg/dL to 88.7 mg/dL) for 9 days.
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Animal Model:NU/NU (8-week-old female) trans-
planted with MDA-MB-468 cells[2] -
Dosage:50 mg/kg
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Administration:i.p.; three times per week; 32 days
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Result:Significantly inhibited tumor growth compared to vehicle control.
Reduced Ki67-positive cells to 150 ± 18 per 1000 tumor cells, representing a decrease compared to vehicle control's 423 ± 27 per 1000 tumor cells.
Showed no significant difference in vimentin staining compared to vehicle control.
Chemical Information
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CAS No. 1515856-92-4
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Appearance Solid
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분자량 366.33
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화학식 C18H17F3N2O3
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Color Off-white to light yellow
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SMILES
O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[C@@H](OCC3=NC=CC=C3)CC2
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Neoplasma
Endothelial lipase promotes acute myeloid leukemia progression through metabolic reprogramming. [Abstract]2022 Jul;69(4):755-763 PMID: 35263993
용액&용해도
DMSO : 100 mg/mL (272.98 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Sun S, et al. Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg Med Chem. 2013;21(24):7724-7734. [Content Brief]
[2]. Lo PK, et al. Inhibition of LIPG phospholipase activity suppresses tumor formation of human basal-like triple-negative breast cancer. Sci Rep. 2020;10(1):8911. Published 2020 Jun 2. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7298 mL | 13.6489 mL | 27.2978 mL | 68.2445 mL |
| 5 mM | 0.5460 mL | 2.7298 mL | 5.4596 mL | 13.6489 mL | |
| 10 mM | 0.2730 mL | 1.3649 mL | 2.7298 mL | 6.8244 mL | |
| 15 mM | 0.1820 mL | 0.9099 mL | 1.8199 mL | 4.5496 mL | |
| 20 mM | 0.1365 mL | 0.6824 mL | 1.3649 mL | 3.4122 mL | |
| 25 mM | 0.1092 mL | 0.5460 mL | 1.0919 mL | 2.7298 mL | |
| 30 mM | 0.0910 mL | 0.4550 mL | 0.9099 mL | 2.2748 mL | |
| 40 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7061 mL | |
| 50 mM | 0.0546 mL | 0.2730 mL | 0.5460 mL | 1.3649 mL | |
| 60 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1374 mL | |
| 80 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8531 mL | |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2730 mL | 0.6824 mL |
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