| CAS NO: | 747412-49-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| 500mg | 询价 |
| Molecular Weight (MW) | 465.54 |
|---|---|
| Formula | C26H31N3O5 |
| CAS No. | 747412-49-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 93 mg/mL (199.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 31 mg/mL (66.6 mM) | |
| Solubility (In vivo) | 1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL |
| Synonyms | Luminespib; NVP AUY922; AUY922; AUY-922; VER52296; VER-52296; NVP AUY-922; NVP-AUY922; NVP-AUY-922; AUY 922; VER 52296 Chemical Name: 5-(2,4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide SMILES Code: O=C(C1=NOC(C2=CC(C(C)C)=C(O)C=C2O)=C1C3=CC=C(CN4CCOCC4)C=C3)NCC |
| In Vitro | In vitro activity: NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 NM. The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of HSP90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. NVP-AUY922 increases the binding of HSP70 to HSP90. NVP-AUY922 causes p23 dissociation from the HSP90 complex and can then recruit HSP70 to the HSP90 complex. After the treatment with NVP-AUY922, expression of receptor tyrosine kinases including VEGFR1, 2, 3 and PDGFRɑ is decreased. A decrease is also noticed in the expression of Akt and phospho-Akt. Meanwhile, treatment with NVP-AUY922 causes decreased expression of HER-2 in NCI-N87 cells. NVP-AUY922 treatment results in binding of HSP90 to client proteins and setting them up as targets for degradation by the proteasome. NVP-AUY922 can influence cell growth by affecting multiple signaling pathways. In addition, treatment with the proteasome inhibitor, MG132, restores expression of thymidylate synthase, which is decreased by NVP-AUY922. NVP-AUY922 increases the expression of cleaved caspase-3 leading to apoptosis in HSC-2 cells. Kinase Assay: NVP-AUY922 is dissolved in DMSO at a concentration of 10 mM. NVP-AUY922 is assessed against HSP90α, HSP90β, GRP94, TRAP-1, HSP72, and topoisomerase II. Profiling against a panel of kinases has been carried out and screening against a panel of additional enzymes and receptors is performed at Cerep. Cell Assay: Human gastric cancer cells NCI-N87 (5-7 ×103 in 50 μL/well) are seeded in 96-well plates and incubated at 37 °C for 24 hours, followed by NVP-AUY922 treatment for 1-3 days at 37 °C. After treatment, the cells are assayed by MTT method and analyzed by microplate reader. |
|---|---|
| In Vivo | Treatment with NVP-AUY922 causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model. In BT474, NVP-AUY922 shows complete loss of ERBB2 and substantial depletion of ERα, in addition to reductions in CDK4 and phospho-ERK1/2. |
| Animal model | Female NCr athymic mice bearing WM266.4 human melanoma xenografts |
| Formulation & Dosage | Dissolved in DMSO and diluted in sterile saline/Tween 20; 50 mg/kg; i.p. and i.v. injection |
| References | Cancer Sci. 2011 Jul;102(7):1388-95; Anticancer Res. 2011 Apr;31(4):1197-204; Cancer Res. 2008 Apr 15;68(8):2850-60. |
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