A selective PAK1 inhibitor
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FRAX1036

Item No. 20711

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[2-chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
1432908-05-8
Molecular Formula
C28H32ClN7O
Formula Weight
518.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlEthanol: 0.33 mg/ml
λmax
211, 299, 308, 355 nm
SMILES
CN1CCC(CCNC2=NC=C(C=C(C3=C(Cl)C=C(C4=NC(C)=CN=C4)C=C3)C(N5CC)=O)C5=N2)CC1
InChi Code
InChI=1S/C28H32ClN7O/c1-4-36-26-21(16-32-28(34-26)31-10-7-19-8-11-35(3)12-9-19)13-23(27(36)37)22-6-5-20(14-24(22)29)25-17-30-15-18(2)33-25/h5-6,13-17,19H,4,7-12H2,1-3H3,(H,31,32,34)
InChi Key
RYCBSFIKWACFBY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $52

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    5 mg

    $227

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    10 mg

    $396

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    25 mg

    $867

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    Product Description

    FRAX1036 is a selective inhibitor of p21-activated kinase 1 (PAK1), a serine/threonine kinase downstream of Rac1 and Cdc42 that is involved in tumorigenesis. It can induce apoptosis in breast cancer cells and has been shown to potentiate the activity of the microtubule stabilizing agent, docetaxel (Item No. 11637).1 Disruption of PAK1 via FRAX1036 has been used to inhibit oncogenic KRAS signaling in non-small cell lung cancer cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ong, C.C., Gierke, S., Pitt, C., et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res. 17:59, (2015).

    2. Mortazavi, F., Lu, J., Phan, R., et al. Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis. BMC Cancer 15(381), (2015).