Alofanib

Modify Date: 2024-01-24 15:57:46

Alofanib Structure
Alofanib structure
Common Name Alofanib
CAS Number 1612888-66-0 Molecular Weight 413.40
Density 1.5±0.1 g/cm3 Boiling Point 659.6±65.0 °C at 760 mmHg
Molecular Formula C19H15N3O6S Melting Point N/A
MSDS N/A Flash Point 352.7±34.3 °C

 Use of Alofanib


Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].

 Names

Name Alofanib
Synonym More Synonyms

 Alofanib Biological Activity

Description Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
Related Catalog
Target

FGFR2

In Vitro Alofanib 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 Vivo In 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

Density 1.5±0.1 g/cm3
Boiling Point 659.6±65.0 °C at 760 mmHg
Molecular Formula C19H15N3O6S
Molecular Weight 413.40
Flash Point 352.7±34.3 °C
Exact Mass 413.068146
LogP 4.00
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.667
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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