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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Cytoskeletal Signaling >HSP e.g. HSP90 inhibitors >PF-04929113

PF-04929113

PF-04929113 Structure
  • ₹0
  • Product name: PF-04929113
  • CAS: 908115-27-5
  • MF: C25H30F3N5O4
  • MW: 521.53
  • EINECS:
  • MDL Number:MFCD20526334
  • Synonyms:(1r,4r)-4-(2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydroindazol-1-yl)phenylamino)cyclohexyl 2-aminoacetate;PF-04929113, >=98%;snx54227;PF04929113 SNX-54227;PF-04929113;SNX-5422;PF-04929113(SNX5422);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
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Properties

Melting point :298-299℃
Boiling point :646.5±55.0 °C(Predicted)
Density :1.48
storage temp. :Store at -20°C
solubility :≥23.85 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
form :solid
pka :15.07±0.50(Predicted)
color :White to off-white

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
Precautionary statements:
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Description

PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM. The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration. 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. Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.

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