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

Theoretical Analysis

MedKoo Cat#: 206428
Name: Alofanib
CAS#: 1612888-66-0
Chemical Formula: C19H15N3O6S
Exact Mass: 413.06816
Molecular Weight: 413.4
Elemental Analysis: C, 55.20; H, 3.66; N, 10.16; O, 23.22; S, 7.76

Size Price Shipping out time Quantity
25mg USD 190 2 Weeks
50mg USD 350 2 Weeks
100mg USD 550 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1850 2 Weeks
1g USD 2950 2 Weeks
2g USD 4650 2 Weeks
5g USD 7850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-24. Prices are subject to change without notice.

Alofanib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 413.4 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.

Select a batch to recalculate based on the batch molecular weight:
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

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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. 2016 Nov 3. [Epub ahead of print] PubMed PMID: 27812884.

2: Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Kochenkov 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. PubMed PMID: 27136102.

3: 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. PubMed PMID: 26732115.

4: 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. PubMed PMID: 26597690.


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