详情描述
Tamatinib, also known as R-406, is a potent inhibitor of Syk with IC50 of 41 nM. R406 impairs platelet activation and monocyte tissue factor expression triggered by heparin-PF4 complex directed antibodies. R406 blocks fc receptor signaling and reduces immune complex-mediated inflammation. R406 inhibited phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 bound to the ATP binding pocket of Syk and inhibited its kinase activity as an ATP-competitive inhibitor (K(i) = 30 nM). R406 blocked Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated activation of B lymphocytes.
Product information
CAS Number: 841290-81-1
Molecular Weight: 628.63
Formula: C28H29FN6O8S
Synonym:
R406 besylate
R406 benzenesulfonate
Related CAS Number:
841290-80-0 (Tamatinib free base)
Chemical Name: 6-((5-fluoro-2-((3, 4, 5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2, 2-dimethyl-2H-pyrido[3, 2-b][1, 4]oxazin-3(4H)-one benzenesulfonate
Smiles: CC1(C)OC2=CC=C(NC3=NC(NC4=CC(OC)=C(OC)C(=C4)OC)=NC=C3F)N=C2NC1=O.OS(=O)(=O)C1C=CC=CC=1
InChiKey: UXDRJPYSTZHIOE-UHFFFAOYSA-N
InChi: InChI=1S/C22H23FN6O5.C6H6O3S/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4;7-10(8,9)6-4-2-1-3-5-6/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30);1-5H,(H,7,8,9)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.