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Lonidamine (CAS 50264-69-2)

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Alternate Names:
1-(2,4-Dichlorobenzyl)-1H-indazole-3-carboxylic acid
Application:
Lonidamine is it elicits cell apoptosis and blocks CFTR Cl- channel
CAS Number:
50264-69-2
Purity:
≥99%
Molecular Weight:
321.16
Molecular Formula:
C15H10Cl2N2O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Lonidamine is an indazole compound that has been reported to inhibit angiogenic-related endothelial cell functions. This compound has been found to trigger apoptosis in endothelial cells and cause a decrease in proliferation, migration, invasion, and morphogenesis. The apoptotic effects of Lonidamine have been demonstrated to be due to Bax, Bid, caspase-3, and caspase-9 activation, as well as cytochrome c release. Futher studies show that Lonidamine prevents cellular energy metabolism via HXK (hexokinase) inhibition. This compound also blocks CFTR Cl- channels in vitro.


Lonidamine (CAS 50264-69-2) References

  1. Recent studies on lonidamine, the lead compound of the antispermatogenic indazol-carboxylic acids.  |  Gatto, MT., et al. 2002. Contraception. 65: 277-8. PMID: 12020777
  2. Mechanism of lonidamine inhibition of the CFTR chloride channel.  |  Gong, X., et al. 2002. Br J Pharmacol. 137: 928-36. PMID: 12411425
  3. Lonidamine: efficacy and safety in clinical trials for the treatment of solid tumors.  |  Di Cosimo, S., et al. 2003. Drugs Today (Barc). 39: 157-74. PMID: 12730701
  4. Lonidamine causes inhibition of angiogenesis-related endothelial cell functions.  |  Del Bufalo, D., et al. 2004. Neoplasia. 6: 513-22. PMID: 15548359
  5. Curcumin stimulates reactive oxygen species production and potentiates apoptosis induction by the antitumor drugs arsenic trioxide and lonidamine in human myeloid leukemia cell lines.  |  Sánchez, Y., et al. 2010. J Pharmacol Exp Ther. 335: 114-23. PMID: 20605902
  6. Reviving Lonidamine and 6-Diazo-5-oxo-L-norleucine to Be Used in Combination for Metabolic Cancer Therapy.  |  Cervantes-Madrid, D., et al. 2015. Biomed Res Int. 2015: 690492. PMID: 26425550
  7. Re-programming tumour cell metabolism to treat cancer: no lone target for lonidamine.  |  Bhutia, YD., et al. 2016. Biochem J. 473: 1503-6. PMID: 27234586
  8. Targeting lonidamine to mitochondria mitigates lung tumorigenesis and brain metastasis.  |  Cheng, G., et al. 2019. Nat Commun. 10: 2205. PMID: 31101821
  9. Targeting glucose metabolism to suppress cancer progression: prospective of anti-glycolytic cancer therapy.  |  Abdel-Wahab, AF., et al. 2019. Pharmacol Res. 150: 104511. PMID: 31678210
  10. Lonidamine potentiates the oncolytic efficiency of M1 virus independent of hexokinase 2 but via inhibition of antiviral immunity.  |  Cai, J., et al. 2020. Cancer Cell Int. 20: 532. PMID: 33292203
  11. Multiple targeted doxorubicin-lonidamine liposomes modified with p-hydroxybenzoic acid and triphenylphosphonium to synergistically treat glioma.  |  Lu, J., et al. 2022. Eur J Med Chem. 230: 114093. PMID: 35007860
  12. Lonidamine and domperidone inhibit expansion of transformed cell areas by modulating motility of surrounding nontransformed cells.  |  Aoyama, M., et al. 2022. J Biol Chem. 298: 102635. PMID: 36273581
  13. Effects of Lonidamine on murine and human tumor cells in vitro. A morphological and biochemical study.  |  De Martino, C., et al. 1984. Oncology. 41 Suppl 1: 15-29. PMID: 6717891

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Lonidamine, 5 mg

sc-203115
5 mg
$105.00

Lonidamine, 25 mg

sc-203115A
25 mg
$364.00

Is there any reccomendation about solvent and solubility please?

Asked by: Yilin
Thank you for your question. This biochemical is soluble in ethanol (5 mM), DMSO (100 mM), CHCl3/MeOH 1/1 (9.80-10.20 mg/ml), water (<1 mg/ml at 25 degrees C), and ethanol (<1 mg/ml at 25 degrees C).
Answered by: Tech Service
Date published: 2019-01-14

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. Lonidamine, sc-203115, is in white to off-white powder form.
Answered by: Chemical Support 4
Date published: 2017-06-21
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Rated 5 out of 5 by from Sanchez et alSanchez et al. (PubMed ID 20605902) found that lonidamine caused mitochondrial transmembrane potential dissipation and apoptosis in human myeloid leukemia cell lines. -SCBT Publication Review
Date published: 2015-04-22
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Lonidamine is rated 5.0 out of 5 by 1.
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