An inhibitor of Aurora A and B kinases
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PF-03814735

Item No. 15015

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide
CAS Number
942487-16-3
Molecular Formula
C23H25F3N6O2
Formula Weight
474.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 16 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:9): 0.10 mg/ml
λmax
203, 240, 275 nm
SMILES
O=C(CNC(C)=O)N1[C@@H](CC[C@H]21)C3=C2C=C(NC4=NC(NC5CCC5)=C(C(F)(F)F)C=N4)C=C3
InChi Code
InChI=1S/C23H25F3N6O2/c1-12(33)27-11-20(34)32-18-7-8-19(32)16-9-14(5-6-15(16)18)30-22-28-10-17(23(24,25)26)21(31-22)29-13-3-2-4-13/h5-6,9-10,13,18-19H,2-4,7-8,11H2,1H3,(H,27,33)(H2,28,29,30,31)/t18-,19+/m0/s1
InChi Key
RYYNGWLOYLRZLK-RBUKOAKNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    50 mg

    $873

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    Product Description

    PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.1 PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.1 PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.1 PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jani, J.P., Arcari, J., Bernardo, V., et al. PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol. Cancer Ther. 9, 883-894 (2010).

    2. Hook, K.E., Garza, S.J., Lira, M.E., et al. An integrated genomic approach to identify predictive biomarkers of response to the aurora kinase inhibitor PF-03814735. Mol. Cancer Ther. 11(3), 710-719 (2012).

    Product Citations

    Small, J.C., Joblin-Mills, A., Carbone, K., et al. Phenotypic screening for small molecules that protect b-cells from glucolipotoxicity. ACS Chem. Biol. 17(5), 1131-1142 (2022).