SSR128129E free acid (Synonyms: SSR free acid)

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

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (SSR128129E) usually boasts enhanced water solubility and stability.

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

SSR128129E free acid Chemical Structure

CAS No. : 848463-13-8

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Other In-stock Forms of SSR128129E free acid:

SSR128129E

Other Forms of SSR128129E free acid:

SSR128129E In-stock

1 Publications Citing Use of MCE SSR128129E free acid

•Cancer Cell. 2021 Jan 11;39(1):68-82.e9. [Abstract]

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Protocol
Purity & Documentation
References
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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].

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

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].

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

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

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

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	[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. [Content Brief]

SSR128129E free acid Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SSR128129E848463-13-8SSRFGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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