| Identification | Back Directory | [Name]
PF-04929113 | [CAS]
908115-27-5 | [Synonyms]
CS-33
snx54227
SNX-5422
PF-04929113
PF-04929113, >=98%
PF-04929113(SNX5422)
PF04929113 SNX-54227
snx5422 PF 04929113
PF-04929113 USP/EP/BP
SNX5422;PF 04929113;SNX 5422;PF-04929113;
(1r,4r)-4-(2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydroindazol-1-yl)phenylamino)cyclohexyl 2-aminoacetate
(1r,4r)-4-((2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl 2-aminoacetate
trans-4-([2-(Aminocarbonyl)-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl] phenyl]amino)cyclohexyl glycinate
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 | [Molecular Formula]
C25H30F3N5O4 | [MDL Number]
MFCD20526334 | [MOL File]
908115-27-5.mol | [Molecular Weight]
521.53 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
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 | [Biological Activity]
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]. | [Enzyme inhibitor]
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. | [in vivo]
SNX-5422 (50 mg/kg, p.o.) efficiently inhibits tumor growth of HT-29 human colon tumor xenograft model after administration 3 times a week for 3 weeks (qod×3/2×3)[1]. SNX-5422 (20, 40 mg/kg, p.o.) markedly inhibits multiple myeloma (MM) tumor growth and angiogenesis in mice[2]. | [target]
Hsp90 | [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. |
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| Company Name: |
NCE Biomedical Co.,Ltd.
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| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
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