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PF-04929113 (SNX-5422)

Catalog No.
A4065
Hsp90 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$132.00
In stock
5mg
$109.00
In stock
10mg
$145.00
In stock
50mg
$455.00
In stock
100mg
$779.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PF-04929113 is an inhibitor of Hsp90 [1].

PF-04929113 is a water soluble and orally bioavailable prodrug of PF-04928473. It is rapidly absorbed and converted into PF-04928473 after oral administration. In mice bearing BT-474 tumor xenografts, treatment of PF-04928473 causes the degradation of the HER2 client protein. And no obvious toxicity is observed when the dose of PF-04928473 is up to 150mg/kg. Treatment of 100mg/kg PF-04928473 results in complete tumor growth inhibition and in some mice partial tumor regressions. PF-04928473 also shows significant antitumor activity in mice with H1650 xenografts. In addition, as an inhibitor of Hsp90, PF-04928473 is reported to inhibit p-ERK and p-Akt, decrease CD31+ cells and MVD as well as a have an effect on angiogenesis in vivo [1, 2].

References:
[1] Chandarlapaty S, Sawai A, Ye Q, Scott A, Silinski M, Huang K, Fadden P, Partdrige J, Hall S, Steed P, Norton L, Rosen N, Solit DB. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res. 2008 Jan 1;14(1):240-8.
[2] Okawa Y, Hideshima T, Steed P, Vallet S, Hall S, Huang K, Rice J, Barabasz A, Foley B, Ikeda H, Raje N, Kiziltepe T, Yasui H, Enatsu S, Anderson KC. 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. 2009 Jan 22;113(4):846-55.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt521.5
Cas No.908115-27-5
FormulaC25H30F3N5O4
Solubility≥23.85 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
Chemical Name[4-[2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]anilino]cyclohexyl] 2-aminoacetate
SDFDownload SDF
Canonical SMILESCC1(CC2=C(C(=O)C1)C(=NN2C3=CC(=C(C=C3)C(=O)N)NC4CCC(CC4)OC(=O)CN)C(F)(F)F)C
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Kinase experiment [1]:

Affinity for Hsp90

Hsp90 from porcine spleen extract was isolated by affinity capture on a purine-affinity media. The Hsp90 loaded media was then challenged with PF-04929113 at a given concentration, ranging from 0.8 to 500 μM, and the amount of Hsp90 liberated at each concentration was determined by Bradford protein assay. The resulting IC50 values were corrected for the ATP ligand concentration and presented as apparent Kd values.
Cell experiment [1]:

Cell lines

MCF-7, SW620, K562, SK-MEL-5 and A375 cancer cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0 ~ 300 nM; 72 or 144 hrs

Applications

In a broad range of cancer cell lines (MCF-7, SW620, K562, SK-MEL-5 and A375 cells), PF-04929113 showed potent antiproliferative activity, with the IC50 values being 16, 19, 23, 25 and 51 nM, respectively.
Animal experiment [2]:

Animal models

Fox Chase SCID mice (6 ~ 7 weeks old) inoculated subcutaneously with 5 × 106 MM.1S cells

Dosage form

20 or 40 mg/kg; p.o.; 3 times per week, for 3 weeks

Applications

PF-04929113 inhibited human MM cell growth and angiogenesis in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Huang KH, Veal JM, Fadden RP, Rice JW, Eaves J, Strachan JP, Barabasz AF, Foley BE, Barta TE, Ma W, Silinski MA, Hu M, Partridge JM, Scott A, DuBois LG, Freed T, Steed PM, Ommen AJ, Smith ED, Hughes PF, Woodward AR, Hanson GJ, McCall WS, Markworth CJ, Hinkley L, Jenks M, Geng L, Lewis M, Otto J, Pronk B, Verleysen K, Hall SE. Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. J Med Chem. 2009 Jul 23;52(14):4288-305.

[2]. Okawa Y, Hideshima T, Steed P, Vallet S, Hall S, Huang K, Rice J, Barabasz A, Foley B, Ikeda H, Raje N, Kiziltepe T, Yasui H, Enatsu S, Anderson KC. 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. 2009 Jan 22;113(4):846-55.

Biological Activity

Description PF-04929113 is a potent and selective inhibitor of Hsp90 with IC50 value of 50 nM.
Targets Hsp90          
IC50 50 nM          

Quality Control

Chemical structure

PF-04929113 (SNX-5422)