1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. SSR128129E free acid

SSR128129E free acid (Synonyms: SSR free acid)

Cat. No.: HY-15599A
Handling Instructions

SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.

For research use only. We do not sell to patients.

SSR128129E free acid Chemical Structure

SSR128129E free acid Chemical Structure

CAS No. : 848463-13-8

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Description

SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.

IC50 & Target[1]

FGFR1

1.9 μM (IC50)

FGFR2

 

FGFR3

 

FGFR4

 

In Vitro

SSR128129E inhibits FGF2-induced EC proliferation with an IC50 of 31±1.6 nM, migration with an IC50 of 15.2±4.5 nM, and lamellipodia formation in a dose dependent manner. SSR128129E inhibits responses mediated by FGFR1-4. For instance, SSR128129E blocks EC migration in response to FGF1, a ligand of FGFR1 and FGFR4, and capillary tube formation in response to FGF19, a ligand of FGFR4. Proliferation and migration of the murine pancreatic Panc02 tumor cell line in response to FGF7 are also blocked by SSR128129E, showing that SSR128129E inhibits FGFR subtypes of other species as well. SSR128129E blocks different FGFR subtypes in various cell lines with nanomolar potency[1].

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].

Molecular Weight

324.33

Formula

C₁₈H₁₆N₂O₄

CAS No.

848463-13-8

SMILES

COC1=C2N(C(C(C3=CC=C(N)C(C(O)=O)=C3)=O)=C1C)C=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

HUVECs, freshly isolated from different donors and used between passage two and five, are cultured in M199 medium supplemented with 20% fetal bovine serum (FBS), 2 mM L-glutamine, 30 mg/L endothelial cell growth factor supplements (EGCS), 10 units/mL heparin, and penicillin/streptomycin. For proliferation, ECs are starved overnight in growth factor-depleted M199 medium containing 2% FBS and stimulated for 24 hr with 10 ng/mL bFGF with SSR128129E or DMSO. Proliferation is assessed the last 2 hr by incubation with 1 μCi/mL [3H]thymidine[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Anesthetized BALB/c mice are inoculated with murine 4T1 mammary carcinoma cells. After randomization of tumor bearing mice for tumor size on day 5 after tumor cell inoculation, SSR128129E or vehicle (0.6 % methylcellulose) is administered daily via oral gavage at a dose of 30 mg/kg until the end of the experiment at day 21. Tumor volume is measured. At the end of the experiment, mice are sacrificed by pentobarbital injection, and lungs and tumors are dissected. Visible metastatic nodules on the lungs are counted by using a dissecting microscope[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

SSR128129ESSRFGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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SSR128129E free acid
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