848463-13-8

Name	FGFR inhibitor
CAS	848463-13-8
Molecular Formula	C18H16N2O4
MDL Number	MFCD25976752
Molecular Weight	324.33
MOL File	848463-13-8.mol

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]-

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Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO

Hazard Information

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

Supplier

SPIRO PHARMA

Telephone

Websitehttp://www.spiropharma.com.cn

Amadis Chemical Company Limited

Telephone571-89925085

Websitehttp://www.amadischem.com

Shanghai Botuo Biotechnology Co., LTD

Telephone 16621358918

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList904553/0_EN.htm

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Telephone13348960310 13348960310

Websitehttps://www.weikeqi-biotech.com/

TargetMol Chemicals Inc.

Telephone4008200310 15002144251

Websitehttps://www.targetmol.cn/

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