SSR128129E
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MedKoo CAT#: 406387

CAS#: 848318-25-2 (sodium)

Description: SSR128129E (SSR) is an potent FGFR inhibitor, which inhibits fibroblast growth factor receptor (FGFR) signaling by binding to the extracellular FGFR domain without affecting orthosteric FGF binding. SSR128129E exhibits allosteric properties, including probe dependence, signaling bias, and ceiling effects. Inhibition by SSR128129E is highly conserved throughout the animal kingdom. Oral delivery of SSR128129E inhibits arthritis and tumors that are relatively refractory to anti-vascular endothelial growth factor receptor-2 antibodies. Thus, orally-active extracellularly acting small-molecule modulators of RTKs with allosteric properties can be developed and may offer opportunities to improve anticancer treatment.

Chemical Structure

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SSR128129E
CAS# 848318-25-2 (sodium)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406387
Name: SSR128129E
CAS#: 848318-25-2 (sodium)
Chemical Formula: C18H16N2O4
Exact Mass: 324.11
Molecular Weight: 324.330
Elemental Analysis: C, 66.66; H, 4.97; N, 8.64; O, 19.73

Price and Availability

Size Price Availability Quantity
10mg USD 110 Ready to ship
25mg USD 220 Ready to ship
50mg USD 385 Ready to ship
100mg USD 685 Ready to ship
200mg USD 1250 Ready to ship
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Related CAS #: 848463-13-8 (free)   848318-25-2 (sodium)    

Synonym: SSR128129E; SSR 128129E; SSR-128129E.

IUPAC/Chemical Name: sodium 2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate

InChi Key: JFBMSTWZURKQOC-UHFFFAOYSA-M

InChi Code: InChI=1S/C18H16N2O4.Na/c1-10-15(20-8-4-3-5-14(20)17(10)24-2)16(21)11-6-7-13(19)12(9-11)18(22)23;/h3-9H,19H2,1-2H3,(H,22,23);/q;+1/p-1

SMILES Code: O=C([O-])C1=CC(C(C2=C(C)C(OC)=C3C=CC=CN23)=O)=CC=C1N.[Na+]

Appearance: Yellow 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, DMF, ethanol, and water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in water

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

More Info:         

Biological target: SSR128129E is a FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
In vitro activity: SSR12819E radiosensitised radioresistant U87 and SF763 glioblastoma cells. SSR128129E administration to U87 cells increased the radiation-induced mitotic cell death. It also decreased cell membrane availability of the FGFR-1 mainly expressed in these cells, increased this receptor's ubiquitylation, inhibited radiation-induced RhoB activation and modulated the level of hypoxia inducible factor, HIF-1α, a master regulator of hypoxia, thus suggesting a role of FGFR in the regulation of hypoxia pathways. Reference: Eur J Cancer. 2014 Sep;50(13):2351-9. https://pubmed.ncbi.nlm.nih.gov/24953334/
In vivo activity: SSR128129E may be a promising drug candidate for the prevention of obesity via suppressing adipogenesis. SSR128129E administration significantly reduced the body weight gain and the fat content of mice. SSR128129E did not increase, but decreased the thermogenic capability of both brown and white fat. However, SSR128129E markedly suppressed adipogenesis of adipose tissues. Reference: Mol Biol Rep. 2022 Sep;49(9):8641-8649. https://pubmed.ncbi.nlm.nih.gov/35731366/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.0 157.25
DMF 30.0 92.50
Ethanol 1.0 3.08
Water 1.0 3.08
PBS (pH 7.2) 1.0 3.08

Preparing Stock Solutions

The following data is based on the product molecular weight 324.33 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.

Recalculate based on batch purity %
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
Formulation protocol: 1. Ader I, Delmas C, Skuli N, Bonnet J, Schaeffer P, Bono F, Cohen-Jonathan-Moyal E, Toulas C. Preclinical evidence that SSR128129E--a novel small-molecule multi-fibroblast growth factor receptor blocker--radiosensitises human glioblastoma. Eur J Cancer. 2014 Sep;50(13):2351-9. doi: 10.1016/j.ejca.2014.05.012. Epub 2014 Jun 18. PMID: 24953334. 2. Zhang X, Wen X, Hu G, Zhang Q, Sun Q, Jia Y, Liu Y, Lin H, Li H. The fibroblast growth factor receptor antagonist SSR128129E inhibits fat accumulation via suppressing adipogenesis in mice. Mol Biol Rep. 2022 Sep;49(9):8641-8649. doi: 10.1007/s11033-022-07699-1. Epub 2022 Jun 22. PMID: 35731366. 3. Bono F, De Smet F, Herbert C, De Bock K, Georgiadou M, Fons P, Tjwa M, Alcouffe C, Ny A, Bianciotto M, Jonckx B, Murakami M, Lanahan AA, Michielsen C, Sibrac D, Dol-Gleizes F, Mazzone M, Zacchigna S, Herault JP, Fischer C, Rigon P, Ruiz de Almodovar C, Claes F, Blanc I, Poesen K, Zhang J, Segura I, Gueguen G, Bordes MF, Lambrechts D, Broussy R, van de Wouwer M, Michaux C, Shimada T, Jean I, Blacher S, Noel A, Motte P, Rom E, Rakic JM, Katsuma S, Schaeffer P, Yayon A, Van Schepdael A, Schwalbe H, Gervasio FL, Carmeliet G, Rozensky J, Dewerchin M, Simons M, Christopoulos A, Herbert JM, Carmeliet P. 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. PMID: 23597562.
In vitro protocol: 1. Ader I, Delmas C, Skuli N, Bonnet J, Schaeffer P, Bono F, Cohen-Jonathan-Moyal E, Toulas C. Preclinical evidence that SSR128129E--a novel small-molecule multi-fibroblast growth factor receptor blocker--radiosensitises human glioblastoma. Eur J Cancer. 2014 Sep;50(13):2351-9. doi: 10.1016/j.ejca.2014.05.012. Epub 2014 Jun 18. PMID: 24953334.
In vivo protocol: 1. Zhang X, Wen X, Hu G, Zhang Q, Sun Q, Jia Y, Liu Y, Lin H, Li H. The fibroblast growth factor receptor antagonist SSR128129E inhibits fat accumulation via suppressing adipogenesis in mice. Mol Biol Rep. 2022 Sep;49(9):8641-8649. doi: 10.1007/s11033-022-07699-1. Epub 2022 Jun 22. PMID: 35731366. 2. Bono F, De Smet F, Herbert C, De Bock K, Georgiadou M, Fons P, Tjwa M, Alcouffe C, Ny A, Bianciotto M, Jonckx B, Murakami M, Lanahan AA, Michielsen C, Sibrac D, Dol-Gleizes F, Mazzone M, Zacchigna S, Herault JP, Fischer C, Rigon P, Ruiz de Almodovar C, Claes F, Blanc I, Poesen K, Zhang J, Segura I, Gueguen G, Bordes MF, Lambrechts D, Broussy R, van de Wouwer M, Michaux C, Shimada T, Jean I, Blacher S, Noel A, Motte P, Rom E, Rakic JM, Katsuma S, Schaeffer P, Yayon A, Van Schepdael A, Schwalbe H, Gervasio FL, Carmeliet G, Rozensky J, Dewerchin M, Simons M, Christopoulos A, Herbert JM, Carmeliet P. 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. PMID: 23597562.

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1: Dol-Gleizes F, Delesque-Touchard N, Marès AM, Nestor AL, Schaeffer P, Bono F. A New Synthetic FGF Receptor Antagonist Inhibits Arteriosclerosis in a Mouse Vein Graft Model and Atherosclerosis in Apolipoprotein E-Deficient Mice. PLoS One. 2013 Nov 4;8(11):e80027. doi: 10.1371/journal.pone.0080027. PubMed PMID: 24224032; PubMed Central PMCID: PMC3817113.

2: Herbert C, Alcouffe C, Bono F. [SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling]. Med Sci (Paris). 2013 Oct;29(10):834-6. doi: 10.1051/medsci/20132910007. Epub 2013 Oct 18. French. PubMed PMID: 24148118.

3: Herbert C, Schieborr U, Saxena K, Juraszek J, De Smet F, Alcouffe C, Bianciotto M, Saladino G, Sibrac D, Kudlinzki D, Sreeramulu S, Brown A, Rigon P, Herault JP, Lassalle G, Blundell TL, Rousseau F, Gils A, Schymkowitz J, Tompa P, Herbert JM, Carmeliet P, Gervasio FL, Schwalbe H, Bono F. Molecular mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling. Cancer Cell. 2013 Apr 15;23(4):489-501. doi: 10.1016/j.ccr.2013.02.018. PubMed PMID: 23597563.

4: Bono F, De Smet F, Herbert C, De Bock K, Georgiadou M, Fons P, Tjwa M, Alcouffe C, Ny A, Bianciotto M, Jonckx B, Murakami M, Lanahan AA, Michielsen C, Sibrac D, Dol-Gleizes F, Mazzone M, Zacchigna S, Herault JP, Fischer C, Rigon P, Ruiz de Almodovar C, Claes F, Blanc I, Poesen K, Zhang J, Segura I, Gueguen G, Bordes MF, Lambrechts D, Broussy R, van de Wouwer M, Michaux C, Shimada T, Jean I, Blacher S, Noel A, Motte P, Rom E, Rakic JM, Katsuma S, Schaeffer P, Yayon A, Van Schepdael A, Schwalbe H, Gervasio FL, Carmeliet G, Rozensky J, Dewerchin M, Simons M, Christopoulos A, Herbert JM, Carmeliet P. 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. PubMed PMID: 23597562.

5: Mohan SK, Rani SG, Chiu IM, Yu C. WITHDRAWN: Interaction of FGF1 with a novel anti-angiogenic drug SSR128129E. Arch Biochem Biophys. 2012 Jun 5. [Epub ahead of print] PubMed PMID: 22683470.