FOSTAMATINIB
r788
CAS: 1025687-58-4
Molecular Formula: C23H24FN6Na2O9P
FOSTAMATINIB - Names and Identifiers
FOSTAMATINIB - Physico-chemical Properties
| Molecular Formula | C23H24FN6Na2O9P |
| Molar Mass | 624.4231642 |
| Melting Point | >191°C (dec.) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Off-White |
| Storage Condition | -20℃ |
| Stability | Hygroscopic |
| Use | R788 (Fostamatinib) Disodium is a prodrug of active metabolite R406. It is a Syk inhibitor with IC50 of 41 nM. It strongly inhibits Syk but does not inhibit Lyn, and has a 5-fold weaker effect on Flt3. Phase 3. |
| In vitro study | R935788 is a prodrug of R406 methylene phosphate that is rapidly converted to R406 in vivo. R406 (the active form of R935788) selectively inhibits Syk-dependent signaling with an EC50 of 33 nM to 171 nM, which is more effective than the Syk-independent pathway. R406 inhibits proliferation of multiple diffuse large B- cell lymphoma (DLBCL) cell lines with an EC50 of 0.8 μm to 8.1 μm. R406 treatment decreased BLNK, Akt, GSK-3, FOXO and ERK phosphorylation. In addition, R406 acts on TCL1 leukemia and completely inhibits anti-IgM antibody-induced BCR signaling. Despite the presence of high levels of constitutively activated Syk in TCL1 leukemia, R406 is not selectively toxic to leukemia cells. |
| In vivo study | Considering that the plasma half-life of R406 in mice is shorter than 2 hours, R935788 is administered in 3 doses, each time separated by 3 hours, to ensure that Syk is continuously suppressed during each administration, mimic longer plasma half-life (15 hours) in humans. Despite relatively mild in vitro cytotoxicity, R935788 significantly inhibits leukemia cell proliferation and survival in vivo, which is associated with blocking antigen-dependent B- cell receptor (BCR) signaling, independent of inhibition of constitutive Syk activity. R935788 treated mice at a dose of 80 mg/kg per day for 18-21 days, effectively inhibited TCL1-002, TCL1-551 and TCL1-870 tumor growth, and no leukemia CD5 was observed at the end of the treatment. |
FOSTAMATINIB - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.601 ml | 8.007 ml | 16.015 ml |
| 5 mM | 0.32 ml | 1.601 ml | 3.203 ml |
| 10 mM | 0.16 ml | 0.801 ml | 1.601 ml |
| 5 mM | 0.032 ml | 0.16 ml | 0.32 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: R788 (Fostamatinib) Disodium Visit Supplier Webpage Request for quotationCAS: 1025687-58-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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