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Key Documents

PZ0209

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C30H33N7O2
CAS Number:
Molecular Weight:
523.63
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Articles

Tec kinases respond to cellular stimulation by various receptors and are involved in signaling pathways.

Tec kinases respond to cellular stimulation by various receptors and are involved in signaling pathways.

Tec kinases respond to cellular stimulation by various receptors and are involved in signaling pathways.

Tec kinases respond to cellular stimulation by various receptors and are involved in signaling pathways.

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