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SSR128129E
Catalog No. T6082Cas No. 848318-25-2
Alias SSR
SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.
SSR128129E
Catalog No. T6082Alias SSRCas No. 848318-25-2
SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $34 | In Stock | |
| 5 mg | $55 | In Stock | |
| 10 mg | $89 | In Stock | |
| 25 mg | $158 | In Stock | |
| 50 mg | $289 | In Stock | |
| 100 mg | $455 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $70 | In Stock |
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Purity:99.21%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 | SSR128129E inhibited FGF2-induced EC proliferation and migration (IC50 =31 nM) and dose-dependently induced cilia formation.SSR128129E inhibited responses mediated by FGFR1-4. For example, SSR128129E blocks the migratory response of cardiomyocytes to FGF1 (ligand for FGFR1 and FGFR4) and the capillary formation response to FGF19 (ligand for FGFR4).
SSR128129E inhibited FGF7-induced proliferation and migration of the murine pancreatic Panc02 tumor cell line, suggesting that SSR128129E also inhibits FGFR isoforms in other species.[1] |
| In vivo | Oral administration of SSR128129E 30 mg/kg/day inhibited the growth of orthotopic Panc02 tumors by 44% starting on day 3 and delayed the growth of Lewis lung cancer. Tumor size and weight were reduced by 53% and 40%, respectively, starting on day 5.[1]
SSR128129E inhibited the growth of subcutaneous CT26 colon tumors and inhibited the growth of a multidrug-resistant MCF7/ADR breast cancer xenograft model.SSR128129E reduced the invasiveness of Panc02 tumor cells and metastasis to peritoneal lymph nodes.[1] |
| 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) |
| Alias | SSR |
| Molecular Weight | 346.31 |
| Formula | C18H15N2O4·Na |
| Cas No. | 848318-25-2 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 1 mg/mL (2.88 mM) DMSO: 45 mg/mL (129.94 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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