Fostamatinib CAS 901119-35-5

Product Description:

Product Name: Fostamatinib CAS 901119-35-5

Synonyms:

FostaMatinib DisodiuM;

6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one.

Chemical & Physical Properties

Appearance:White to Off-White solid

Assay: NLT98%

Molecular Formula:C23H26FN6O9P

Molecular Weight:580.46

Melting point:214℃~ 217℃

Boiling point:814.2±75.0℃(Predicted)

Density:1.496

Storage temp:-20℃, Hygroscopic

Solubility:DMSO (Slightly), Methanol (Slightly)

Pka:1.70±0.10(Predicted)

Vapour Pressure:0.0±3.1 mmHg at 25℃

Index of Refraction:1.629

Uses :

In vitro: R788 is a methylene phosphate prodrug of R406, which can be rapidly converted to R406 in vivo: R406 (in vitro active form of R788) selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells. R406 inhibits cellular proliferation of a variety of diffuse large B-cell lymphoma (DLBCL) cell lines with EC50 values ranging from 0.8 μM to 8.1 μM . R406 treatment reduces basal phosphorylation of BLNK, Akt, glycogen synthase kinase-3 (GSK-3), forkhead box O (FOXO) and ERK not only in cells with high (TCL-002) but also in cells with low levels of phosphorylated Syk (TCL1-551). In addition, R406 completely inhibits the anti-IgM induced Bcr signal in TCL1 leukemias. Despite the higher levels of constitutively active Syk in TCL1 leukemias, R406 is not selectively cytotoxic to the leukemic cells.

In vivo: R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals.

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