R406 is an orally bioavailable and selective inhibitor of spleen tyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30 nM. R406 is an active component of its prodrug R788 or R935788 (Fostamatinib).
Mol Med Rep. 2018 Aug 3.
In vitro and in vivo study of the expression of the Syk/Ras/c‑Fos pathway in chronic glomerulonephritis.
R-406 purchased from AbMole
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Source | Molecular Medicine Reports (2018). Figure 5. R406 (Abmole Bioscience) |
| Method | HBZY - 1 cell model establishment | |
| Cell Lines | HBZY - 1 cell | |
| Concentrations | 1.5 µg/ml | |
| Incubation Time | 48 h | |
| Results | The inhibitor R406 inhibited the LPS-induced activation of the Syk/Ras/c-Fos signaling pathway. |
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Source | Molecular Medicine Reports (2018). Figure 4. R406 (Abmole Bioscience) |
| Method | HBZY - 1 cell model establishment | |
| Cell Lines | HBZY - 1 cell | |
| Concentrations | 1.5 µg/ml | |
| Incubation Time | 48 h | |
| Results | Furthermore, R406 was revealed to inhibit the LPS-induced activation of the Syk/Ras/c-Fos signaling pathway. |
| Cell Experiment | |
|---|---|
| Cell lines | CLL cells |
| Preparation method | To evaluate the effect of BCR stimulation on CLL cell viability, CLL cells (107/mL) were incubated in complete RPMI medium (control) or in complete medium supplemented with 10 μg/mL anti-IgM (polyclonal goat F(ab′)2 fragments to human IgM [MP Biomedicals] at 37°C in 5% CO2). After 24 and 48 hours, CLL cell viability was measured by analysis of mitochondrial transmembrane potential by 3,3 dihexyloxocarbocyanine iodine (DiOC6; Invitrogen-Molecular Probes) and cell membrane permeability to propidium iodide (PI; Molecular Probes), as described.13 Briefly, 200 μL cell suspension was collected at the indicated time points and transferred to fluorescence-activated cell sorter tubes containing 200 μL of 60 nM DiOC6 and 2 μg/mL PI in RPMI with 0.5% bovine serum albumin. Cells were then incubated at 37°C for 15 minutes and analyzed within 30 minutes by flow cytometry on a FACSCalibur (BD Biosciences). |
| Concentrations | 5 μM |
| Incubation time | 24 and 48 h |
| Animal Experiment | |
|---|---|
| Animal models | K/BxN Model in C57BL/6 mice |
| Formulation | 35% TPGS, 60% PEG 400, and 5% propylene glycol |
| Dosages | b.i.d for 13 days |
| Administration | orally |
| Molecular Weight | 470.45 |
| Formula | C22H23FN6O5 |
| CAS Number | 841290-80-0 |
| Solubility (25°C) | DMSO 11 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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R343 is an immunoglobulin E (IgE) as well as spleen tyrosine kinase (Syk) inhibitor for studies related to allergic asthma and non-small cell lung cancer. |
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