A PAK1 inhibitor
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AZ 13705339

Item No. 42087

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[[2-[[3-(ethylsulfonyl)-4-(4-methyl-1-piperazinyl)phenyl]amino]-5-fluoro-4-pyrimidinyl][5-(hydroxymethyl)-2-methylphenyl]amino]methyl]-benzonitrile
CAS Number
2016806-57-6
Molecular Formula
C33H36FN7O3S
Formula Weight
629.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
FC1=CN=C(NC2=CC=C(N3CCN(CC3)C)C(S(=O)(CC)=O)=C2)N=C1N(CC4=CC=CC=C4C#N)C5=C(C)C=CC(CO)=C5
InChi Code
InChI=1S/C33H36FN7O3S/c1-4-45(43,44)31-18-27(11-12-29(31)40-15-13-39(3)14-16-40)37-33-36-20-28(34)32(38-33)41(21-26-8-6-5-7-25(26)19-35)30-17-24(22-42)10-9-23(30)2/h5-12,17-18,20,42H,4,13-16,21-22H2,1-3H3,(H,36,37,38)
InChi Key
WPFLVPJXKWCRQK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

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    25 mg

    $290

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    50 mg

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    Product Description

    AZ 13705339 is an inhibitor of p21-activated kinase 1 (PAK1; IC50 = 0.33 nM).1 It is selective for PAK1 over a panel of 117 kinases at 100 nM. AZ 13705339 binds to PAK1 and PAK2 (Kd = 0.28 and 0.32 nM, respectively). It inhibits S. enterica infection in HAP1 chronic myeloid leukemia cells when used at a concentration of 10 µM.2 AZ 13705339 inhibits cell death induced by an antibody targeting sialic acid binding Ig-like lectin 8 (Siglec-8) in IL-5-stimulated primary human eosinophils (IC50 = 59 nM).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McCoull, W., Hennessy, E.J., Blades, K., et al. Optimization of highly kinase selective bis-anilino pyrimidine PAK1 inhibitors. ACS Med. Chem. Lett. 7(12), 1118-1123 (2016).

    2. Davidson, A., Tyler, J., Hume, P., et al. A kinase-independent function of PAK is crucial for pathogen-mediated actin remodelling. PLoS Pathog. 17(8), e1009902 (2021).

    3. Carroll, D.J., Cao, Y., Bochner, B.S., et al. Siglec-8 signals through a non-canonical pathway to cause human eosinophil death in vitro. Front. Immunol. 12, 737988 (2021).