PZ0209

PF-06465469

≥97% (HPLC)

• Synonym(s): 3-[4-Amino-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-N-[3-methyl-4-(1-methylethyl)phenyl]-benzamide
• Empirical Formula (Hill Notation): C₃₀H₃₃N₇O₂
• CAS Number: 1407966-77-1
• Molecular Weight: 523.63
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥97% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 5 mg/mL, clear
• storage temp.: 2-8°C
• InChI: 1S/C30H33N7O2/c1-5-25(38)36-13-7-10-23(16-36)37-29-26(28(31)32-17-33-29)27(35-37)20-8-6-9-21(15-20)30(39)34-22-11-12-24(18(2)3)19(4)14-22/h5-6,8-9,11-12,14-15,17-18,23H,1,7,10,13,16H2,2-4H3,(H,34,39)(H2,31,32,33)/t23-/m1/s1
• InChI key: CGJVMKJGKFEHTL-HSZRJFAPSA-N

Description

Biochem/physiol Actions

PF-06465469 is a potent, covalent inhibitor of the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase), which is expressed primarily in immune cells, and is strongly upregulated following activation of T-cells. PF-06465469 inhibits Itk enzymatic activity with an IC₅₀ of 2 nM. The compound blocks anti-CD3 induced phosphorylation of PLCg in Jurkat cells (IC₅₀ = 31 nM) and IL-2 production in anti-CD3 stimulated human whole blood (IC₅₀ = 48 nM).

Features and Benefits

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Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H315,H319,H335
• pcodes: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• target_organs: Respiratory system
• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable