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[CAS NO. 50264-69-2] Lonidamine
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-B0486 |
| Brand: | MCE |
| CAS: | 50264-69-2 |
Overview
| MDL | MFCD00866285 |
|---|---|
| Molecular Weight | 321.16 |
| Molecular Formula | C15H10Cl2N2O2 |
| SMILES | O=C(C1=NN(CC2=CC=C(Cl)C=C2Cl)C3=C1C=CC=C3)O |
5 Publications Citing Use of MCE
Summary
Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor ( K i : 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis [1] [2] [3] .
IC50 & Target
Ki: 2.5 μM (Mitochondrial pyruvate carrier) [2]
In Vitro
Lonidamine (100 μM, 24 h) inhibits TGF-β-stimulated lactate production and oxygen consumption rate in AKR-2B and TIG-1 cells
[3]
.
Lonidamine (100 μM, 24/48 h) inhibits H2030BrM3 and A549 cell proliferation
[4]
.
Lonidamine (100-200 μM, 24 h) inhibits H2030BrM3 and A549 cell invasion
[4]
.
Lonidamine (100-1000 μM, 24 h) inhibits mitochondrial complex I and II activities
[4]
.
Lonidamine (200 μM, 24 h) increases ROS generation in H2030BrM3 lung cancer cells
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model
[3]
.
|
| Dosage: | 10, 30, 100 mg/kg/day |
| Administration: | Oral administration, daily, d10 to d20 after BLM treatment. |
| Result: | Partially or completely reversed the increases in HK2 and lactate induced by BLM and reduced the expression of 10 profibrotic mediators. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00435448 | Threshold Pharmaceuticals|PRA Health Sciences |
Benign Prostatic Hyperplasia|Enlarged Prostate
|
June 2005 | Phase 3 |
| NCT00237536 | Threshold Pharmaceuticals |
Benign Prostatic Hyperplasia
|
June 2005 | Phase 2 |
Appearance
Solid
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
DMSO : 50 mg/mL ( 155.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1137 mL | 15.5686 mL | 31.1371 mL |
| 5 mM | 0.6227 mL | 3.1137 mL | 6.2274 mL |
| 10 mM | 0.3114 mL | 1.5569 mL | 3.1137 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution
References
- [1] Nancolas B, et al. The anti-tumour agent lonidamine is a potent inhibitor of the mitochondrial pyruvate carrier and plasma membrane monocarboxylate transporters. Biochem J. 2016 Apr 1;473(7):929-36.
- [2] Ilya A Shutkov, et al. Ru(III) Complexes with Lonidamine-Modified Ligands. Int J Mol Sci. 2021 Dec 15;22(24):13468.
- [3] Xueqian Yin, et al. Hexokinase 2 couples glycolysis with the profibrotic actions of TGF-β. Sci Signal. 2019 Dec 17;12(612):eaax4067.
- [4] Gang Cheng, et al. Targeting lonidamine to mitochondria mitigates lung tumorigenesis and brain metastasis. Nat Commun. 2019 May 17;10(1):2205.
Synonyms
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