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Luminespib (NVP-AUY922) Europäischer Partner

ArtNr S1069-10mM
Hersteller Selleckchem
CAS-Nr. 747412-49-3
Menge 10 mM/1 mL
Quantity options 10 mg 1 g 10 g 100 mg 10 mM/1 mL 200 mg 25 mg 5 mg 5 g
Kategorie
Typ Inhibitors
Specific against other
Smiles CCNC(=O)C1=NOC(=C1C2=CC=C(C=C2)CN3CCOCC3)C4=CC(=C(C=C4O)O)C(C)C
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias AUY-922,VER-52296
Similar products AUY922
Lieferbar
Storage Conditions
2 years -80 in solvent
Molecular Weight
465, 54
Administration
Administered via i.v. or i.p.
Animal Models
Female NCr athymic mice bearing WM266.4 human melanoma xenografts
Cell lines
Human gastric cancer cells NCI-N87
Concentrations
1 uM
Dosages
50 mg/kg
Formulation
In DMSO and diluted in sterile saline/Tween 20
IC50
13 nM, 13 nM, 13 nM, 13 nM, 13 nM, 13 nM
In vitro
NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. [1] 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. [1] After the treatment with NVP-AUY922, expression of receptor tyrosine kinases including VEGFR1, 2, 3 and PDGFR 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 mutiple 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.[1]
In vivo
Treatment with NVP-AUY922 causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model. [2] In BT474, NVP-AUY922 shows complete loss of ERBB2 and substantial depletion of ERalpha, in addition to reductions in CDK4 and phospho-ERK1/2. [3]
Incubation Time
3 days
Kinase Assay
[3], Kinase assay, NVP-AUY922 is dissolved in DMSO at a concentration of 10 mM. NVP-AUY922 is assessed against HSP90alpha, HSP90beta, 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.
Method
Human gastric cancer cells NCI-N87 (5-7 x103 in 50 uL/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.
Solubility (25C)
DMSO 93 mg/mL, Water <1 mg/mL, Ethanol 93 mg/mL
Information
Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Chemical Name
5-(2, 4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 10 mM/1 mL
Lieferbar: In stock
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