SML4053

R406

≥98% (HPLC)

• Synonym(s): 6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one, N4-(2,2-dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, R 406 (free base), Tamatinib (free base)
• Empirical Formula (Hill Notation): C₂₂H₂₃FN₆O₅
• CAS Number: 841290-80-0
• Molecular Weight: 470.45
• MDL number: MFCD27976370
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Warmed)
• storage temp.: -10 to -25°C
• SMILES string: CC1(C(NC2=C(O1)C=CC(NC3=NC(NC4=CC(OC)=C(C(OC)=C4)OC)=NC=C3F)=N2)=O)C
• InChI: 1S/C22H23FN6O5/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/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30)
• InChI key: NHHQJBCNYHBUSI-UHFFFAOYSA-N

Description

Biochem/physiol Actions

Orally available, potent, and selective ATP competitive inhibitor of Syk (spleen tyrosine kinase); TAK1 activator.
R406 (Tamatinib) is an orally available, potent, and selective ATP competitive inhibitor of Syk (spleen tyrosine kinase) activity (Ki= 30 nM). R406 potently induces apoptosis in cancer cells overexpressing Syk. R406 is the active metabolite of pro-drug Fostamatinib (R-788). R406 promotes the activation of TAK1 by direct binding to TAK1, independent of its original target Syk kinase.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable