A pan-Pim kinase inhibitor
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CX-6258

Item No. 16245

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3E)-5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one
CAS Number
1202916-90-2
Synonyms
  • Pim-Kinase Inhibitor X
Molecular Formula
C26H24ClN3O3
Formula Weight
461.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/ml
λmax
212, 258, 403 nm
SMILES
O=C(N1CCCN(C)CC1)C2=CC=CC(C3=CC=C(/C=C4C(NC5=C/4C=C(Cl)C=C5)=O)O3)=C2
InChi Code
InChI=1S/C26H24ClN3O3/c1-29-10-3-11-30(13-12-29)26(32)18-5-2-4-17(14-18)24-9-7-20(33-24)16-22-21-15-19(27)6-8-23(21)28-25(22)31/h2,4-9,14-16H,3,10-13H2,1H3,(H,28,31)/b22-16+
InChi Key
KGBPLKOPSFDBOX-CJLVFECKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $106

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    10 mg

    $185

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    25 mg

    $392

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    Product Description

    CX-6258 is a potent, reversible inhibitor of Pim-1, -2, and -3 (IC50s = 5, 25, and 16 nM, respectively).1 It demonstrates excellent selectivity, inhibiting only FLT3 from a panel of 107 additional kinases. CX-6258 dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1.1,2 It acts synergistically with the chemotherapeutics doxorubicin and paclitaxel, presumably because CX-6258 impairs Pim-mediated enhanced expression of P-glycoprotein.1 CX-6258 is orally bioavailable and inhibits the growth of MV4-11 xenografts in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Haddach, M., Michaux, J., Schwaebe, M.K., et al. Discovery of CX-6258. A potent, selective, and orally efficacious pan-Pim kinases inhibitor. ACS Med. Chem. Lett. 3(2), 135-139 (2011).

    2. Padmanabhan, A., Gosc, E.B., and Bieberich, C.J. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J. Cell. Biochem. 114, 1050-1057 (2013).