A pan-Aurora kinase and Abl inhibitor
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Danusertib

Item No. 18387

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-methyl-1-piperazinyl)-N-[1,4,5,6-tetrahydro-5-[(2R)-2-methoxy-2-phenylacetyl]pyrrolo[3,4-c]pyrazol-3-yl]-benzamide
CAS Number
827318-97-8
Synonyms
  • PHA-739358
Molecular Formula
C26H30N6O3
Formula Weight
474.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 20 mg/mlEthanol: 25 mg/ml
λmax
310 nm
SMILES
CN1CCN(C2=CC=C(C(NC3=NNC4=C3CN(C([C@H](OC)C5=CC=CC=C5)=O)C4)=O)C=C2)CC1
InChi Code
InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1
InChi Key
XKFTZKGMDDZMJI-HSZRJFAPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $147

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    10 mg

    $230

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    50 mg

    $627

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    Product Description

    Danusertib is a pan-Aurora kinase inhibitor (IC50s = 13, 79, and 61 nM for Aurora A, B, and C, respectively) that also targets Abl, Ret, TrkA and FGFR1 (IC50s = 25, 31, 31, and 47 nM, respectively).1 It exhibits anti-proliferative and pro-apoptotic activity against a panel of cancer cells in vitro, including those expressing wild type and mutant Bcr-Abl.1,2 Danusertib is effective against diverse xenografts in mice, including those containing mutant Bcr-Abl that are resistant to imatinib (Item No. 13139).1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Carpinelli, P., Ceruti, R., Giorgini, M.L., et al. PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol. Cancer Ther. 6(12 Pt 1), 3158-3153 (2007).

    2. Gontarewicz, A., Balabanov, S., Keller, G., et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. Blood 111(8), 4355-4364 (2008).

    3. Moore, A.S., Blagg, J., Linardopoulos, S., et al. Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias. Leukemia 24(4), 671-678 (2010).