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PF-04929113

Cat. No. M2003
PF-04929113 Structure
Synonym:

SNX-5422

Size Price Availability Quantity
10mg USD 370 In stock
50mg USD 855 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PF-04929113 is a small-molecule Hsp90 inhibitor based on the 6,7-dihydro-indazol-4-one scaffold. PF-04929113 also inhibits Her-2 degradation with IC50 of 37 nM. PF-04929113 inhibited tumor growth and prolonged survival compared with controls. Surprisingly, PF-04929113 did not reduce serum prostate-specific antigen (PSA) levels in vivo; in parallel, these decrease in tumor volume. PF-04929113 administered orally twice a week is well tolerated and inhibits its intended target Hsp90. PF-04929113 is currently under the Phase I clinical trial.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 521.53
Formula C25H30F3N5O4
CAS Number 908115-27-5
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

A phase I study of PF-04929113 (SNX-5422), an orally bioavailable heat shock protein 90 inhibitor, in patients with refractory solid tumor malignancies and lymphomas.
Rajan A, et al. Clin Cancer Res. 2011 Nov 1;17(21):6831-9. PMID: 21908572.

A novel HSP90 inhibitor delays castrate-resistant prostate cancer without altering serum PSA levels and inhibits osteoclastogenesis.
Lamoureux F, et al. Clin Cancer Res. 2011 Apr 15;17(8):2301-13. PMID: 21349995.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-04929113, SNX-5422 supplier, HSP90, inhibitors

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