| Fostamatinib (R788)Spleen tyrosine kinase (Syk) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.15%
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Chemical structure
Related Biological Data
Related Biological Data
| Cell experiment [1]: | |
Cell lines | Diffuse large B-cell lymphoma (DLBCL) cell lines |
Preparation method | The solubility of this compound in DMSO is > 100.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 4 μM, 96 h |
Applications | R788 was a prodrug of the active metabolite. R406 induced apoptosis of the majority of examined DLBCL cell lines. In R406-sensitive DLBCL cell lines, R406 specifically inhibited both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYK-dependent phosphorylation of the B-cell linker protein [BLNK]). |
| Animal experiment [2]: | |
Animal models | Eμ- TCL1 transgenic mouse model of CLL, B6/C3H F1 mice |
Dosage form | Intraperitoneal administration, 18 consecutive days at a daily dose of 80 mg/kg |
Application | R788 (80 mg/kg/d) inhibited the growth of adoptively transferred TCL1 leukemias in vivo. R788 treatment administered from days 4 to 25 after adoptive transfer significantly prevented the outgrowth of leukemias. Treatment with R788 significantly prolonged the survival of the animals. In B6/C3H mice, after 4 days of treatment animals receiving R788 showed a greater rise in the number of circulating malignant lymphocytes than controls. In B6/C3H F1 mice, treatment with R788 for 7 days blocked BCR signaling and inhibited leukemic cell survival and proliferation in vivo. In Eμ- TCL1 transgenic mouse model of CLL, R788 inhibited the growth of spontaneously developing TCL1 leukemias. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Chen L, Monti S, Juszczynski P, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma[J]. Blood, 2008, 111(4): 2230-2237. [2]. Suljagic M, Longo P G, Bennardo S, et al. The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Eμ-TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling[J]. Blood, 2010, 116(23): 4894-4905. | |
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| Cas No. | 901119-35-5 | SDF | Download SDF |
| Chemical Name | [6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate | ||
| Canonical SMILES | CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)(O)O)C | ||
| Formula | C23H26FN6O9P | M.Wt | 580.46 |
| Solubility | ≥100.4mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Fostamatinib is a small molecule inhibitor of spleen tyrosine kinase (Syk) with IC50 value of 41nM [1].
Fostamatinib is an orally bioavailable prodrug of R406. It is developed for the treatment of autoimmune diseases. The effective metabolite of fostamatinib, R406, is an ATP-competitive inhibitor of Syk with Ki value of 30nM. R406 also inhibits the activity of other kinases including Flt3, Lyn (IC50=63nM) and Lck (IC50=37nM). It is found that R406 inhibits both BCR and FcR mediated responses in vitro. Besides that, R406 also shows effects in other cells types and signalling pathways. In the in vivo assay, fostamatinib shows to be highly active to inhibit FcR-mediated signaling in various animal models of allergy, autoimmunity and inflammation. Moreover, fostamatinib also exerts efficacy in SLE animal models. Treatment of fostamatinib suppresses the established renal and skin disease and reduces lymphadenopathy in the MRL/lpr strain [1].
References:[1] McAdoo S P, Tam F W K. Fostamatinib disodium. Drugs of the future, 2011, 36(4): 273.
