Fostamatinib(R788)

产品编号: DC9841 Featured
Fostamatinib(R788)
结构式
901119-35-5
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中国地区超过5000个高品质化合物库存
应用领域
Fostamatinib (R788) 是R406的活性代谢物的原药,是Syk抑制剂,IC50为41 nM。
Cas No.: 901119-35-5
名称:
别名: R 788,R-788,R788
SMILES: COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O)(O)=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC
分子式: C23H26FN6O9P
分子量: 580.46
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC9841 Fostamatinib(R788) Fostamatinib (R788) 是R406的活性代谢物的原药,是Syk抑制剂,IC50为41 nM。
DC1013 R788 disodium (Fostamatinib) Fostamatinib Disodium (R788 Disodium) 是活性代谢物R406的原药,是Syk抑制剂,IC50为41 nM。