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SSR128129E

Catalog No. T6082 CAS 848318-25-2

Synonyms: SSR

SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.

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SSR128129E, CAS 848318-25-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 158.00
50 mg	In stock	$ 289.00
100 mg	In stock	$ 455.00
1 mL * 10 mM (in DMSO)	In stock	$ 70.00

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Purity: 99.21%

Purity: 98.79%

Purity: 98%

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Description	SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.
Targets&IC50	FGFR1:1.9 μM
In vitro	In various murine tumor models, SSR128129E (30 mg/kg, p.o.) demonstrated the ability to inhibit both the proliferation and metastasis of primary tumors. Additionally, in mice with arthritis, SSR128129E (30 mg/kg, p.o.) reduced inflammation, angiogenesis, and bone resorption, thereby alleviating clinical symptoms. Furthermore, SSR128129E also inhibited the proliferation of both resistant and sensitive strains in models of tumors with anti-vascular endothelial growth factor receptor 2 activity, enhancing the anti-tumor activity against the vascular endothelial growth factor receptor 2.
In vivo	Due to its allosteric mechanism, SSR128129E exhibits enhanced activity in cell assays. It inhibits FGF2-induced proliferation and migration of endothelial cells in a dose-dependent manner, with an IC50 of 31/15.2 nM. As a multitarget fibroblast growth factor receptor (FGFR) inhibitor, SSR128129E blocks responses mediated by FGFR1-4, thus inhibiting proliferation and/or migration across various cell lines, including mPanc02, HEK-hFGFR2WT, PAE-hFGFR1, hB9-myeloma, and human umbilical vein endothelial cell lines.
Kinase Assay	Scintillation Proximity Assay, 125I-FGF-2 Binding: SPA protein A beads are supplied as a suspension in PBS at 20 mg/mL, then diluted with binding buffer (KCl, 400 mg/L; MgSO4 200 mg/L; NaCl 6.4 g/L; NaHCO3 3.7 g/L; NaH2PO4 0.141 mg/mL; bis Tris Propane 11.292 g/L; Glucose 4.5 g/L; Gelatin 0.1 %; pH 7.0) at 10 mg/mL. 125I-FGF-2 radioligand and FGFR-1IIIc? - Fc Chimera are diluted into binding buffer. Binding was performed on 96-well plates coated with 0.1 % gelatin. Total assay volume is 0.1 mL. Binding of 125I-FGF-2 is determined by incubation of SPA beads coated with protein A (0.5 mg/assay) with FGFR-1IIIc? - Fc chimera soluble receptor (5 ng/assay), FGF-2 (20 ng/assay) is used for non-specific binding determinations.
Cell Research	Cell proliferation of porcine aortic endothelial (PAE) and tumor cell lines is analyzed on exponentially growing cells that are starved for 16 hours in 0.2 % FBS containing medium and seeded at 4,000 cells/well in 96-well microplates. After exposure to mitogens and/or SSR for 72 hours, cell proliferation is assessed with the use of the CellTiter 96 AQueous One Solution Cell Proliferation Assay according to manufacturer’s instructions. 10 % FBS containing medium is used a positive control. (Only for Reference)

Synonyms	SSR
Molecular Weight	346.31
Formula	C18H15N2O4·Na
CAS No.	848318-25-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 1 mg/mL (2.88 mM)

DMSO: 64 mg/mL (184.8 mM)

References and Literature

1. Bono F, et al. Cancer Cell. 2013, 23(4), 477-488. 2. Dol-Gleizes F, et al. PLoS One. 2013, 8(11), e820027.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Compound Library NO PAINS Compound Library Anti-Liver Cancer Compound Library Anti-Fibrosis Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library

Related Products

Related compounds with same targets

Fazpilodemab Ferulic acid sodium FGFR1 inhibitor-10 PD-161570 ZM323881 hydrochloride Nintedanib esylate PD173074 TAK-632

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Keywords

SSR128129E 848318-25-2 Angiogenesis Tyrosine Kinase/Adaptors FGFR SSR-128129E SSR Fibroblast growth factor receptor Inhibitor inhibit inhibitor

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