Alofanib
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MedKoo CAT#: 206428

CAS#: 1612888-66-0

Description: Alofanib, also known as RPT835, is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity. Alofanib blocks the extracellular part of the receptor and prevents its binding with the ligand. Alofanib suppressed proliferation of endothelial cells, their migration activity, and ability to form vessellike structures in vitro and significantly decreased the number of microvessels in Matrigel implant and in ovarian cancer (SKOV-3) xenograft in vivo. RPT835 potently inhibited growth of KATO III gastric cancer cells expressing FGFR2, with GI50 value of 10 nmol/L.

Chemical Structure

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Alofanib
CAS# 1612888-66-0
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206428
Name: Alofanib
CAS#: 1612888-66-0
Chemical Formula: C19H15N3O6S
Exact Mass: 413.07
Molecular Weight: 413.400
Elemental Analysis: C, 55.20; H, 3.66; N, 10.16; O, 23.22; S, 7.76

Price and Availability

Size Price Availability Quantity
25mg USD 150 2 Weeks
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1650 2 Weeks
1g USD 2950 2 Weeks
2g USD 5250 2 Weeks
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Synonym: RPT835; RPT-835; RPT 835; Alofanib

IUPAC/Chemical Name: 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid

InChi Key: QUQGQIASFYWKAB-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H15N3O6S/c1-12-8-18(22(25)26)17(10-16(12)14-5-3-7-20-11-14)21-29(27,28)15-6-2-4-13(9-15)19(23)24/h2-11,21H,1H3,(H,23,24)

SMILES Code: O=[N+](C1=CC(C)=C(C2=CC=CN=C2)C=C1NS(=O)(C3=CC(C(O)=O)=CC=C3)=O)[O-]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
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Biological target: Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2).
In vitro activity: Alofanib was evaluated for antiproliferative activity against the human ovarian cancer FGFR-expressing cell line in FGF-mediated signaling model. FGF2 significantly increased proliferation of the ovarian cancer cells in untreated control group (P = 0.001). Cells were treated with increasing concentrations of alofanib ranging from 0 to 1 μmol/L. Compound significantly inhibited FGF-triggered cell proliferation in dose-dependent manner (P < 0.001). To find out whether alofanib could demonstrate cytotoxic activity in vitro, this study examined the effect of compound on SKOV3 cell line by MTT assay. Alofanib displayed low cytotoxic effect on ovarian cancer cells. Compound inhibited growth of SKOV3 cells with GI50 value of 0.37 μmol/L (Fig. 2a). Reference: Invest New Drugs. 2017 Apr;35(2):127-133. https://pubmed.ncbi.nlm.nih.gov/27812884/
In vivo activity: Ability of alofanib to block tumor angiogenesis in vivo in tumors was evaluated on the model of human serous ovarian cancer SKOV-3 inoculated to mice with immune deficiency. Peroral administration of alofanib (50 mg/kg) reduced the number of CD31+ microvessels in tumor tissue by 48.9% in comparison with the control (p<0.001, Table 2). Histological analysis revealed significant dilatation and plethora of tumor microvessels and extensive hemorrhages. Reference: Bull Exp Biol Med. 2015 Nov;160(1):84-7. https://pubmed.ncbi.nlm.nih.gov/26597690/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.7 115.38
DMSO:PBS (pH 7.2) (1:6) 0.1 0.34
DMF 30.0 72.57

Preparing Stock Solutions

The following data is based on the product molecular weight 413.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Tyulyandina A, Harrison D, Yin W, Stepanova E, Kochenkov D, Solomko E, Peretolchina N, Daeyaert F, Joos JB, Van Aken K, Byakhov M, Gavrilova E, Tjulandin S, Tsimafeyeu I. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2017 Apr;35(2):127-133. doi: 10.1007/s10637-016-0404-1. Epub 2016 Nov 3. PMID: 27812884. 2. Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Khochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W, Ryabaya O, Byakhov M, Tjulandin S. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8. doi: 10.1016/j.ejca.2016.03.068. Epub 2016 Apr 29. Erratum in: Eur J Cancer. 2017 Jan;70:156. PMID: 27136102. 3. Khochenkov DA, Solomko ES, Peretolchina NM, Ryabaya OO, Stepanova EV. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7. doi: 10.1007/s10517-015-3104-5. Epub 2015 Nov 24. PMID: 26597690.
In vitro protocol: 1. Tyulyandina A, Harrison D, Yin W, Stepanova E, Kochenkov D, Solomko E, Peretolchina N, Daeyaert F, Joos JB, Van Aken K, Byakhov M, Gavrilova E, Tjulandin S, Tsimafeyeu I. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2017 Apr;35(2):127-133. doi: 10.1007/s10637-016-0404-1. Epub 2016 Nov 3. PMID: 27812884. 2. Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Khochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W, Ryabaya O, Byakhov M, Tjulandin S. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8. doi: 10.1016/j.ejca.2016.03.068. Epub 2016 Apr 29. Erratum in: Eur J Cancer. 2017 Jan;70:156. PMID: 27136102.
In vivo protocol: 1. Tyulyandina A, Harrison D, Yin W, Stepanova E, Kochenkov D, Solomko E, Peretolchina N, Daeyaert F, Joos JB, Van Aken K, Byakhov M, Gavrilova E, Tjulandin S, Tsimafeyeu I. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2017 Apr;35(2):127-133. doi: 10.1007/s10637-016-0404-1. Epub 2016 Nov 3. PMID: 27812884. 2. Khochenkov DA, Solomko ES, Peretolchina NM, Ryabaya OO, Stepanova EV. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7. doi: 10.1007/s10517-015-3104-5. Epub 2015 Nov 24. PMID: 26597690.

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1: Tyulyandina A, Harrison D, Yin W, Stepanova E, Kochenkov D, Solomko E, Peretolchina N, Daeyaert F, Joos JB, Van Aken K, Byakhov M, Gavrilova E, Tjulandin S, Tsimafeyeu I. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2017 Apr;35(2):127-133. doi: 10.1007/s10637-016-0404-1. Epub 2016 Nov 3. PMID: 27812884.


2: Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Khochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W, Ryabaya O, Byakhov M, Tjulandin S. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8. doi: 10.1016/j.ejca.2016.03.068. Epub 2016 Apr 29. Erratum in: Eur J Cancer. 2017 Jan;70:156. PMID: 27136102.


3: Khochenkov DA, Solomko ES, Peretolchina NM, Ryabaya OO, Stepanova EV. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7. doi: 10.1007/s10517-015-3104-5. Epub 2015 Nov 24. PMID: 26597690.


4: Tsimafeyeu I, Statsenko G, Vladimirova L, Besova N, Artamonova E, Raskin G, Rykov I, Mochalova A, Utyashev I, Gorbacheva S, Kazey V, Gavrilova E, Dragun N, Moiseyenko V, Tjulandin S. A phase 1b study of the allosteric extracellular FGFR2 inhibitor alofanib in patients with pretreated advanced gastric cancer. Invest New Drugs. 2023 Apr;41(2):324-332. doi: 10.1007/s10637-023-01340-z. Epub 2023 Mar 13. PMID: 36907947.


5: Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Khochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W, Ryabaya O, Byakhov M, Tjulandin S. Corrigendum to 'Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models' [Eur J Cancer 61 (2016) 20-28]. Eur J Cancer. 2017 Jan;70:156. doi: 10.1016/j.ejca.2016.11.001. Epub 2016 Dec 3. Erratum for: Eur J Cancer. 2016 Jul;61:20-8. PMID: 27919550.


6: Tsimafeyeu I, Daeyaert F, Joos JB, Aken KV, Ludes-Meyers J, Byakhov M, Tjulandin S. Molecular Modeling, de novo Design and Synthesis of a Novel, Extracellular Binding Fibroblast Growth Factor Receptor 2 Inhibitor Alofanib (RPT835). Med Chem. 2016;12(4):303-17. doi: 10.2174/1573406412666160106154726. PMID: 26732115.