| Identification | Back Directory | [Name]
FGFR inhibitor | [CAS]
848463-13-8 | [Synonyms]
SSR free acid
FGFR inhibitor
SSR128129E free acid
SSR-128129E free acid
SSR128129E (free base)
Benzoic acid, 2-amino-5-[(1-methoxy-2-methyl-3-indolizinyl)carbonyl]- | [Molecular Formula]
C18H16N2O4 | [MDL Number]
MFCD25976752 | [MOL File]
848463-13-8.mol | [Molecular Weight]
324.33 |
| Hazard Information | Back Directory | [Uses]
SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1. | [Definition]
ChEBI: 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoic acid is an aminobenzoic acid that is anthranilic acid substituted at position 5 by a (1-methoxy-2-methylindolizin-3-yl)carbonyl group. It has a role as an antineoplastic agent and a fibroblast growth factor receptor antagonist. It is a member of indolizines, an aminobenzoic acid, an aromatic ether and an aromatic ketone. It is functionally related to an anthranilic acid. It is a conjugate acid of a 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoate. | [in vivo]
Oral delivery of SSR128129E (30 mg/kg/day, from day 3) inhibits growth of orthotopic Panc02 tumors by 44% and delays growth of Lewis lung carcinoma. oral SSR128129E (30 mg/kg/day, from day 5) reduces tumor size and weight by 53% and 40%, respectively. SSR128129E inhibits the growth of subcutaneous CT26 colon tumors by 34% and of the multidrug resistant MCF7/ADR breast cancer xenograft model by 40%. SSR128129E reduces tumor invasiveness and metastasis of Panc02 tumor cells to peritoneal lymph nodes[1]. | [IC 50]
FGFR1: 1.9 μM (IC50); FGFR2; FGFR3; FGFR4 | [References]
[1] Bono F, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013 Apr 15;23(4):477-88. DOI:10.1016/j.ccr.2013.02.019 |
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SPIRO PHARMA
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www.spiropharma.com.cn |
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Musechem
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www.musechem.com |
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cjbscvictory
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https://www.weikeqi-biotech.com/ |
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