| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
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 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. |
| 产品描述 | 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: |
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