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福他替尼 (R788), 酪氨酸蛋白激酶 SYK 抑制剂

福他替尼 (R788), 酪氨酸蛋白激酶 SYK 抑制剂

规格或纯度: ≥98%

CAS编号: 901119-35-5
分子式: C₂₃H₂₆FN₆O₉P
分子量: 580.46
PubChem编号: 11671467

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货号 (SKU)	包装规格	是否现货	价格	数量
F129915-5mg	5mg	现货
F129915-10mg	10mg	现货
F129915-25mg	25mg	现货
F129915-50mg	50mg	现货

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基本描述

英文别名	Fostamatinib\|901119-35-5\|R788\|Fostamatinib (R788)\|Tavlesse\|R788 compound\|Tavalisse\|R-935788 Free acid\|Fostamatinib(R788)\|R-788 Free acid\|R935788 FREE ACID\|R788 FREE ACID\|R 788\|R-788\|[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimeth
规格或纯度	≥98%
英文名称	Fostamatinib (R788)
生化机理	R788 (Fostamatinib) is an important spleen tyrosine kinase (Syk) inhibitor, showing efficacy against kinase-mediated IgG Fc gamma receptor signaling. R788 inhibits the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage. In one study, inhibition of BCR signaling with R788 affected the growth of certain leukemia cell lines. These leukemia cells express stereotyped BCRs that react with auto-antigens exposed on the surface of senescent or apoptotic cells, sμggesting that they are antigen driven.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Fostamatinib (R788)是活性代谢产物R406的前体药物，是一种Syk抑制剂，IC50为41 nM，强效抑制Syk但不抑制Lyn，对Flt3作用效果低5倍。Phase 3。An inhibitor to spleenic kinase-mediated IgG Fc receptor signaling Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3. An inhibitor to spleenic kinase-mediated IgG Fc receptor signaling

产品属性

ALogP	1.6

名称和标识符

IUPAC Name	[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate
INCHI	InChI=1S/C23H26FN6O9P/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29)
InChi Key	GKDRMWXFWHEQQT-UHFFFAOYSA-N
Canonical SMILES	CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)(O)O)C
Isomeric SMILES	CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)(O)O)C
PubChem CID	11671467
分子量	580.46

数据库链接

Wikipedia	Fostamatinib
PubChem CID	11671467
ChEMBL Ligand	CHEMBL2103830
CAS Registry No.	901119-35-5
RCSB PDB Ligand	2RC
DrugCentral Ligand	5280

化学和物理性质

溶解性	DMSO 116 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

安全和危险性（GHS）

象形图	Harmful
信号词	Warning
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation H335: May cause respiratory irritation
预防措施声明	P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P264+P265,P337+P317,P332+P317,P319

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参考文献

1. Braselmann S, Taylor V, Zhao H, Wang S, Sylvain C, Baluom M, Qu K, Herlaar E, Lau A, Young C et al.. (2006) R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.. J Pharmacol Exp Ther, 319 (3): (998-1008). [PMID:16946104]
2. Sweeny DJ, Li W, Clough J, Bhamidipati S, Singh R, Park G, Baluom M, Grossbard E, Lau DT. (2010) Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation.. Drug Metab Dispos, 38 (7): (1166-76). [PMID:20371637]
3. Kunwar S, Devkota AR, Ghimire DK. (2016) Fostamatinib, an oral spleen tyrosine kinase inhibitor, in the treatment of rheumatoid arthritis: a meta-analysis of randomized controlled trials.. Rheumatol Int, 36 (8): (1077-87). [PMID:27113955]
4. Maringwa J, Kågedal M, Hamrén UW, Martin P, Cox E, Hamrén B. (2015) Pharmacokinetic-pharmacodynamic modeling of fostamatinib efficacy on ACR20 to support dose selection in patients with rheumatoid arthritis (RA).. J Clin Pharmacol, 55 (3): (328-35). [PMID:25280085]
5. Newland A, Lee EJ, McDonald V, Bussel JB. (2018) Fostamatinib for persistent/chronic adult immune thrombocytopenia.. Immunotherapy, 10 (1): (9-25). [PMID:28967793]
6. Niscola P, Scaramucci L, Giovannini M. (2018) Spleen tyrosine kinase inhibition: a new promising approach to chronic and refractory immune thrombocytopenia.. Immunotherapy, 10 (1): (5-7). [PMID:29192558]

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