受注:045-509-1970 |
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Synonyms | SSR | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H15N2O4.Na |
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分子量 | 346.31 | CAS No. | 848318-25-2 | |
Solubility (25°C)* | 体外 | DMSO | 69 mg/mL (199.24 mM) | |
Water | 1 mg/mL (2.88 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs. |
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in vitro | SSR128129E exhibits more effective activity in cell assay due to its allosteric mechanism. SSR128129E dose-dependently inhibits FGF2-induced EC proliferation and migration with IC50 of 31 nM and 15.2 nM, respectively. As a multi-FGFR inhibitor, SSR128129E inhibits responses mediated by FGFR1-4 and thus results in the blockage of proliferation and/or migration in various cell lines including mPanc02, HEK-hFGFR2WT, PAE-hFGFR1, hB9-myeloma and HUVEC. [1] |
in vivo | In Arthritis mice, SSR128129E (30 mg/kg, p.o.) inhibits angiogenesis, inflammation, and bone resorption, and reduces the severity of clinical symptoms. In mice bearing various tumor models, SSR128129E (30 mg/kg, p.o.) inhibits both the growth of primary tumors and metastasis. In addition, SSR128129E inhibits growth of anti-VEGFR2-refractory and -sensitive tumor models, and enhances the antitumor activity of anti-VEGFR2. [1] SSR128129E also inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice. [2] |
キナーゼアッセイ | Scintillation Proximity Assay, 125I-FGF-2 Binding | |
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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-1IIIcß - 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-1IIIcß - Fc chimera soluble receptor (5 ng/assay), FGF-2 (20 ng/assay) is used for non-specific binding determinations. | ||
細胞アッセイ | 細胞株 | Endothelial cells (ECs) and Panc02 tumor cells |
濃度 | ~100 nM | |
反応時間 | 72 hours | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Mouse model of Arthritic and mouse tumor model bearing pancreatic tumor cell line Panc02, murine mammary carcinoma cell line 4T1, murine colon cancer cell line CT26, or human breast MCF7/ADR cell line. |
投薬量 | ~30 mg/kg | |
投与方法 | Oral administration |
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Data from [Data independently produced by , , Exp Mol Med, 2017, 49(9):e374]
Data from [Data independently produced by , , Oncogenesis, 2017, 6(1):e285]
FGF-2 promotes angiogenesis through a SRSF1/SRSF3/SRPK1-dependent axis that controls VEGFR1 splicing in endothelial cells [ BMC Biol, 2021, 19(1):173] | PubMed: 34433435 |
MEKK1 Regulates Chemokine Expression in Mammary Fibroblasts: Implications for the Breast Tumor Microenvironment [ Front Oncol, 2021, 11:609918] | PubMed: 33868996 |
Extracellular vesicles from human airway basal cells respond to cigarette smoke extract and affect vascular endothelial cells [ Sci Rep, 2021, 11(1):6104] | PubMed: 33731767 |
Cisplatin Resistance in Osteosarcoma: In vitro Validation of Candidate DNA Repair-Related Therapeutic Targets and Drugs for Tailored Treatments. [ Front Oncol, 2020, 10;10:331] | PubMed: 32211337 |
VEGF pathway-targeting drugs induce evasive adaptation by activation of neuropilin-1/cMet in colon cancer cells. [ Int J Oncol, 2018, 52(4):1350-1362] | PubMed: 29532881 |
API5 induces cisplatin resistance through FGFR signaling in human cancer cells. [Jang HS, et al. Exp Mol Med, 2017, 49(9):e374] | PubMed: 28883546 |
API5 confers cancer stem cell-like properties through the FGF2-NANOG axis. [Song KH, et al. Oncogenesis, 2017, 6(1):e285] | PubMed: 28092370 |
Ferulic Acid Exerts Anti-Angiogenic and Anti-Tumor Activity by Targeting Fibroblast Growth Factor Receptor 1-Mediated Angiogenesis. [ Int J Mol Sci, 2015, 16(10):24011-31] | PubMed: 26473837 |
Integration of signals along orthogonal axes of the vertebrate neural tube controls progenitor competence and increases cell diversity [ PLoS Biol, 2014, 12(7):e1001907] | PubMed: 25026549 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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