LonidamineIt elicits cell apoptosis and blocks CFTR Cl- channel

Lonidamine (CAS 50264-69-2)

Lonidamine | CAS 50264-69-2 is rated 5.0 out of 5 by 1.
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Synonym: 1-(2,4-Dichlorobenzyl)-1H-indazole-3-carboxylic acid
Application: It elicits cell apoptosis and blocks CFTR Cl- channel
CAS Number: 50264-69-2
Purity: ≥99%
Molecular Weight: 321.16
Molecular Formula: C15H10Cl2N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

1. De Martino, C., et al. 1984. Oncology. 41: 15-29. PMID: 6717891
2. Gong, X., et al. 2002. Br. J. Pharmacol. 137: 928-936. PMID: 12411425
3. Del Bufalo, D., et al. 2004. Neoplasia. 6: 513-522. PMID: 15548359
4. Sánchez, Y., et al. 2010. J. Pharmacol. Exp. Ther. 335: 114-123. PMID: 20605902

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in ethanol (5 mM), DMSO (100 mM), CHCl3/MeOH 1/1 (9.80-10.20 mg/ml), water (<1 mg/ml at 25° C), DMSO (64 mg/ml at 25° C), and ethanol (<1 mg/ml at 25° C).
Storage :
Store at room temperature
Melting Point :
198.17° C (Predicted)
Boiling Point :
537.93° C at 760 mmHg (Predicted)
Density :
1.48 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
M17 leucyl aminopeptidas: IC50 = 7.37 µM (Plasmodium falciparum 3D7)
pK Values :
pKa: 3 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
NK7886000
PubChem CID :
39562
MDL Number :
MFCD00866285
EC Number :
256-510-0
Beilstein Registry :
894483
SMILES :
C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O

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Certificate of Analysis

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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 (&lt;1 mg/ml at 25 degrees C), and ethanol (&lt;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 al Sanchez 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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