PF-04929113

Bezeichnung:PF-04929113

CAS-Nr908115-27-5

Englisch Name:PF-04929113

CBNumberCB52561489

SummenformelC25H30F3N5O4

Molgewicht521.53

MOL-Datei908115-27-5.mol

PF-04929113 physikalisch-chemischer Eigenschaften

Schmelzpunkt	298-299℃
Siedepunkt	646.5±55.0 °C(Predicted)
Dichte	1.48
storage temp.	Store at -20°C
Löslichkeit	≥23.85 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
Aggregatzustand	solid
pka	15.07±0.50(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

PF-04929113 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
PF 04929113 can be used in pharmacological activity and therapeutic use in therapeutic breast cancer drug target for multiclass comparative virtual screening to identify novel Hsp90 inhibitors. HSP90
Biologische Aktivität
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].
Enzyminhibitor
This potent and selective HSP90 inhibitor (FW = 521.54 g/mol; CAS 908115-27-5; Solubility: 100 mg/mL DMSO, <1mg/mL H2O), also knownas SNX-5422 and (1R,4R)-4-(2-carbamoyl-5-(6,6-dimethyl-4-oxo-3- (trifluoromethyl)-4,5,6,7-tetrahydroindazol-1-yl)phenylamino)cyclohexyl 2- aminoacetate, targets heat shock protein-90 (Kd = 41 nM) and also inhibits Her-2 degradation (IC50 = 37 nM). PF-04929113 also shows potent antiproliferative activity against a broad range of cancer cell types, e.g. MCF-7 (IC50 =16 nM), SW620 (IC50 =19 nM), K562 (IC50 =23 nM), SK-MEL-5 (IC50 =25 nM), and A375 (IC50 =51 nM). SNX2112 inhibits in vitro proliferation, inducing G2/M arrest, and enhanced cytotoxicity, chemosensitivity, and radiosensitivity between 25 and 250 nM, decreasing expression and/or phosphorylation of EGFR, c-MET, AKT, ERK-1 and -2, IκB kinase, and STAT3, corresponding downstream NFκB, AP-1, and STAT3 reporter genes, and target oncogenes and angiogenic cytokines.
target
Hsp90
Einzelnachweise
[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.

PF-04929113 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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