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Alofanib

Catalog No. T5122 CAS 1612888-66-0

Synonyms: RPT835

Alofanib (RPT835) is a selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect on FGF2-induced phosphorylation of FRS2a in KATO III cells (IC50 <10 nM). It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.

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Alofanib, CAS 1612888-66-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 213.00
50 mg	In stock	$ 318.00
100 mg	In stock	$ 493.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.53%

Purity: 99.06%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Alofanib (RPT835) is a selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect on FGF2-induced phosphorylation of FRS2a in KATO III cells (IC50 <10 nM). It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
Targets&IC50	FGFR2:<10 nM
In vitro	In SKOV3 cell line, Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2. It has a low cytotoxic effect on ovarian cancer cells [1]. Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumor types (triple-negative breast cancer, melanoma, and ovarian cancer), alofanib inhibits FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose-dependently inhibits the proliferation and migration of human and mouse endothelial cells (GI50: 11-58 nmol/l) compared with brivanib and bevacizumab [2].
In vivo	Alofanib (i.v.) significantly in a dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. Alofanib suppresses angiogenesis in the ovarian cancer mouse model[1]. In an FGFR-driven human tumor xenograft model, oral administration of alofanib is well tolerated and results in potent antitumor activity[2].
Cell Research	SKOV3 cells were treated with alofanib (10, 100, and 1000 μM) for 72 h and whole-cell lysates were immunoblotted.

Synonyms	RPT835
Molecular Weight	413.4
Formula	C19H15N3O6S
CAS No.	1612888-66-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 55 mg/mL (133.04 mM)

References and Literature

1. Tyulyandina A, et al. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2017 Apr;35(2):127-133. 2. Tsimafeyeu I, et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8.

Citations

1. Sun K, Sun J, Yan C, et al.Sympathetic Neurotransmitter, VIP, Delays Intervertebral Disc Degeneration via FGF18/FGFR2‐Mediated Activation of Akt Signaling Pathway.Advanced Biology.2023: 2300250.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Preclinical Compound Library Anti-Liver Cancer Compound Library Anti-Lung Cancer Compound Library

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Keywords

Alofanib 1612888-66-0 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR RPT 835 Inhibitor inhibit RPT-835 RPT835 Fibroblast growth factor receptor inhibitor

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