CAS 1612888-66-0|Alofanib

Introduction:Basic information about CAS 1612888-66-0|Alofanib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameAlofanib
CAS Number1612888-66-0Molecular Weight413.40
Density1.5±0.1 g/cm3Boiling Point659.6±65.0 °C at 760 mmHg
Molecular FormulaC19H15N3O6SMelting Point/
MSDS/Flash Point352.7±34.3 °C

Names

NameAlofanib
SynonymMore Synonyms

Alofanib BiologicalActivity

DescriptionAlofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
Related CatalogResearch Areas >>CancerResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>Protein Tyrosine Kinase/RTK >>FGFR
Target

FGFR2

In VitroAlofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in cancer cells expressing different FGFR2 isoforms[1]. Alofanib (10-1000 nM) inhibits FGF-mediated proliferation in a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer with GI50s of 16-370 nM[1].
In VivoIn a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg) is well tolerated and resulted in potent antitumour activity[1]. Treatment with alofanib ablated experimental FGF-induced angiogenesis in vivo[1].
References

[1]. Tsimafeyeu I, et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8.

[2]. Khochenkov DA, et al. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7.

Chemical & Physical Properties

Density1.5±0.1 g/cm3
Boiling Point659.6±65.0 °C at 760 mmHg
Molecular FormulaC19H15N3O6S
Molecular Weight413.40
Flash Point352.7±34.3 °C
Exact Mass413.068146
LogP4.00
Vapour Pressure0.0±2.1 mmHg at 25°C
Index of Refraction1.667
InChIKeyQUQGQIASFYWKAB-UHFFFAOYSA-N
SMILESCc1cc([N+](=O)[O-])c(NS(=O)(=O)c2cccc(C(=O)O)c2)cc1-c1cccnc1
Storage condition-20℃

Synonyms

3-{[4-Methyl-2-nitro-5-(3-pyridinyl)phenyl]sulfamoyl}benzoic acid
Benzoic acid, 3-[[[4-methyl-2-nitro-5-(3-pyridinyl)phenyl]amino]sulfonyl]-
Alofanib (RPT835)
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