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NVP-HSP990

Cat. No. M1798
NVP-HSP990 Structure
Synonym:

HSP990

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 600 In stock
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Quality Control
Biological Activity

NVP-HSP990, as a novel oral Hsp90 inhibitor, has been developed and characterized in vitro and in vivo. In vitro, NVP-HSP990 exhibits single digit nanomolar IC(50) values on three of the Hsp90 isoforms (Hsp90α, Hsp90β, and GRP94) and 320 nanomolar IC(50) value on the fourth (TRAP-1), with selectivity against unrelated enzymes, receptors, and kinases. In c-Met amplified GTL-16 gastric tumor cells, NVP-HSP990 dissociated the Hsp90-p23 complex, depleted client protein c-Met, and induced Hsp70. NVP-HSP990 potently inhibited the growth of human cell lines and primary patient samples from a variety of tumor types. In vivo, NVP-HSP990 exhibits drug-like pharmaceutical and pharmacologic properties with high oral bioavailability. In the GTL-16 xenograft model, a single oral administration of 15 mg/kg of NVP-HSP990 induced sustained downregulation of c-Met and upregulation of Hsp70. In repeat dosing studies, NVP-HSP990 treatment resulted in tumor growth inhibition of GTL-16 and other human tumor xenograft models driven by well-defined oncogenic Hsp90 client proteins. On the basis of its pharmacologic profile and broad-spectrum antitumor activities, clinical trials have been initiated to evaluate NVP-HSP990 in advanced solid tumors.

Protocol
Cell Experiment
Cell lines GTL-16, BT-474, A549, NCI-H1975 and MV4;11 cell lines
Preparation method Cell proliferation and apoptosis assays Cells were treated with NVP-HSP990 or 17-AAG for 72 hours, and cell viability was determined by CellTiter-Glo Luminescent Cell Viability assay from Promega. Soft agar clonogenic assays with primary human tumors were conducted at Oncotest GmbH
Concentrations 0~1000nM
Incubation time 72 h
Animal Experiment
Animal models Human tumor xenograft models GTL-16, NCI-H1975, BT474, and MV4;11
Formulation 100% polyethylene glycol (PEG400)
Dosages a single dose of 15 mg/kg
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 379.39
Formula C20H18FN5O2
CAS Number 934343-74-5
Purity >99%
Solubility DMSO
Storage at -20°C
References

The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo.
Menezes DL, et al. Mol Cancer Ther. 2012 Mar;11(3):730-9. PMID: 22246440.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NVP-HSP990, HSP990 supplier, HSP90, inhibitors

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