A prodrug for an Hsp90 inhibitor
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Active Metabolite(s)
22359SNX-2112
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PF-04929113

Item No. 18270

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
glycine, trans-4-[[2-(aminocarbonyl)-5-[4,5,6,7-tetrahydro-6,6-dimethyl-4-oxo-3-(trifluoromethyl)-1H-indazol-1-yl]phenyl]amino]cyclohexyl ester
CAS Number
908115-27-5
Synonyms
  • SNX-5422
Molecular Formula
C25H30F3N5O4
Formula Weight
521.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.25 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
250, 359 nm
SMILES
O=C(CN)O[C@@H](CC1)CC[C@H]1NC2=CC(N3N=C(C(F)(F)F)C4=C3CC(C)(C)CC4=O)=CC=C2C(N)=O
InChi Code
InChI=1S/C25H30F3N5O4/c1-24(2)10-18-21(19(34)11-24)22(25(26,27)28)32-33(18)14-5-8-16(23(30)36)17(9-14)31-13-3-6-15(7-4-13)37-20(35)12-29/h5,8-9,13,15,31H,3-4,6-7,10-12,29H2,1-2H3,(H2,30,36)/t13-,15-
InChi Key
AVDSOVJPJZVBTC-CTYIDZIISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $484

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    25 mg

    $1,060

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    Cayman Chemical
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    Product Description

    PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04928473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.1,2 The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.2 The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.1,3 Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chandarlapaty, S., Sawai, A., Ye, Q., et al. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin. Cancer Res. 14(1), 240-248 (2008).

    2. Jain, L., Gardner, E.R., Venitz, J., et al. Determination of PF-04928473 in human plasma using liquid chromatography with tandem mass spectrometry. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 878(30), 3187-3192 (2010).

    3. Okawa, Y., Hideshima, T., Steed, P., et al. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood 113(4), 846-855 (2009).

    4. Lamoureux, F., Thomas, C., Yin, M.J., et al. A novel HSP90 inhibitor delays castrate-resistant prostate cancer without altering serum PSA levels and inhibits osteoclastogenesis. Clin. Cancer Res. 17(8), 2301-2313 (2011).