Alofanib - CAS 1612888-66-0
Catalog number: B0084-470877
Category: Inhibitor
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Molecular Formula:
C19H15N3O6S
Molecular Weight:
413.404
COA:
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Targets:
FGFR
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.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-470877 10 mg $899 In stock
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Purity:
95%
Appearance:
Solid Powder
Synonyms:
RPT835; RPT-835
Solubility:
Soluble in DMSO, not in water
MSDS:
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Shelf Life:
2 years
InChIKey:
QUQGQIASFYWKAB-UHFFFAOYSA-N
InChI:
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)
Canonical SMILES:
CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]
1.Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models.
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 Eur J Cancer. 2016 Jul;61:20-8. doi: 10.1016/j.ejca.2016.03.068. Epub 2016 Apr 29.
Alofanib (RPT835) is a novel selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). We showed previously that alofanib could bind to the extracellular domain of FGFR2 and has an inhibitory effect on FGF2-induced phoshphorylation of FRS2α. In the present study, we further showed that alofanib inhibited phosphorylation of FRS2α with the half maximal inhibitory concentration (IC50) values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer), alofanib inhibited FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose dependently inhibited the proliferation and migration of human and mouse endothelial cells (GI50 11-58 nmol/l) compared with brivanib and bevacizumab. Treatment with alofanib ablated experimental FGF-induced angiogenesis in vivo. In a FGFR-driven human tumour xenograft model, oral administration of alofanib was well tolerated and resulted in potent antitumour activity. Importantly, alofanib was effective in FGFR2-expressing models. These results show that alofanib is a potent FGFR2 inhibitor and provide strong rationale for its evaluation in patients with FGFR2-driven cancers.
2.Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies.
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 Invest New Drugs. 2017 Apr;35(2):127-133. doi: 10.1007/s10637-016-0404-1. Epub 2016 Nov 3.
Purpose Early data suggest that combining FGFR2 inhibitors with platinum-containing cytotoxic agents for the treatment of epithelial ovarian cancer may yield increased antitumor activity. We investigated antitumor activity of alofanib (RPT835), a novel allosteric FGFR2 inhibitor, in ovarian cancer in vitro and in vivo. Methods Equal amounts of ovarian cancer cell (SKOV3) lysates were analyzed for FGFR1-3 protein expression using Wes. To assess the efficacy of alofanib on FGF-mediated cell proliferation, SKOV3 cells were incubated and were treated with serially diluted alofanib. Basic FGF was added at a concentration of 25 ng/ml. Control wells were left untreated. Cell growth inhibition was determined using Promega's Cell Titer-Glo® assay. Immunocompromised mice were used for xenotransplantation of SKOV3 cancer cells. Seventy animals with measurable tumors were selected on day 10 and randomized into control groups (no treatment or chemotherapy alone (paclitaxel + carboplatin) and treatment groups (alofanib orally or intravenously (different dose levels) in combination with chemotherapy). Measurements of tumor volume (mm3) were performed by digital calipers every 3 days during 31 days after tumor inoculation.
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CAS 1612888-66-0 Alofanib

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