Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H15N3O6S |
| Molecular Weight | 413.404 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(=C(NS(=O)(=O)C2=CC(=CC=C2)C(O)=O)C=C1C3=CN=CC=C3)[N+]([O-])=O
InChI
InChIKey=QUQGQIASFYWKAB-UHFFFAOYSA-N
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)
Russian Pharmaceutical Technologies is developing alofanib, a first in class, allosteric inhibitor of fibroblast growth factor receptor type 2 (FGFR2) for the treatment of tumours expressing FGFR2, including ovarian cancer, colorectal cancer and lung cancer. Alofanib is a potential allosteric inhibitor of FGFR2 used in oncology. Alofanib has potent effects on ovarian cancer growth in preclinical studies.The inhibitor 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. The results indicate that Alofanib can inhibit angiogenesis.
Approval Year
Sample Use Guides
Mice: Daily intravenous regimen of alofanib (total maximum dose per week was 350 mg/kg) demonstrated significant effect (inhibiting growth by 80 % and by 53 % in comparison with vehicle and chemotherapy group alone, respectively
Route of Administration:
Intravenous
Alofanib is an allosteric inhibitor of FGFR2 and significantly inhibited bFGF-induced proliferation of HUVEC cells (IC50 value of 11 nM) and suppressed proliferation of SVEC-4-10 cells (IC50 value of 58 nM).
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 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).
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86280646
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10171
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C170744
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300000037034
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1612888-66-0
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LQX7RFK8MZ
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admin on Sat Dec 16 11:27:03 GMT 2023 , Edited by admin on Sat Dec 16 11:27:03 GMT 2023
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ACTIVE MOIETY
