An Itk covalent inhibitor
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PF-06465469

Item No. 31118

Product Insert (PDF)
Technical Information
Formal Name
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
CAS Number
1407966-77-1
Molecular Formula
C30H33N7O2
Formula Weight
523.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/ml
SMILES
NC1=C(C(C2=CC=CC(C(NC3=CC(C)=C(C(C)C)C=C3)=O)=C2)=NN4[C@@]5([H])CN(C(C=C)=O)CCC5)C4=NC=N1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $109

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    10 mg

    $207

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    25 mg

    $491

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    50 mg

    $818

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    Product Description

    PF-06465469 is a covalent inhibitor of IL-2-inducible T cell kinase (Itk; IC50 = 2 nM).1 It also inhibits Bruton's tyrosine kinase (BTK; IC50 = 2 nM). PF-06465469 inhibits Itk phosphorylation of phospholipase Cγ (PLCγ) induced by an anti-CD3 antibody in Jurkat cells (IC50 = 57 nM). It induces apoptosis in Jurkat cells, MOLT-4 and CCRF CEM T cell lymphoblasts, and Karpas-299 large cell lymphoma cells when used at a concentration of 16 µM.2 PF-06465469 (2 µM) inhibits chemotaxis induced by chemokine (C-X-C motif) ligand 12 (CXCL12) in Jurkat cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zapf, C.W., Gerstenberger, B.S., Xing, L., et al. Covalent inhibitors of interleukin-2 inducible T cell kinase (Itk) with nanomolar potency in a whole-blood assay. J. Med. Chem. 55(22), 10047-10063 (2012).

    2. Mamand, S., Allchin, R.L., Ahearne, M.J., et al. Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma. Sci. Rep. 8(1), 14216 (2018).