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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

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About This Item

Empirical Formula (Hill Notation):
C30H33N7O2
CAS Number:
1407966-77-1
Molecular Weight:
523.63
UNSPSC Code:
12352200
NACRES:
NA.77
eCl@ss:
32160703
Assay:
≥97% (HPLC)
Form:
powder
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Quality Segment

assay

≥97% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear

storage temp.

2-8°C

SMILES string

N1(C[C@@H](CCC1)[n]2nc(c5c2ncnc5N)c3cc(ccc3)C(=O)Nc4cc(c(cc4)C(C)C)C)C(=O)C=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).
PF-06465469 is a potent, covalent inhibitor of the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase).

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
GHS07

Signal Word

Warning

Hazard Codes

H315,H319,H335

Hazard Classifications

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

Target Organs

Respiratory system

Storage Class

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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