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NVP-HSP990

Catalog No. T6118 CAS 934343-74-5

Synonyms: HSP990

NVP-HSP990 (HSP990) is an effective and specific HSP90α/β inhibitor (IC50: 0.6 /0.8 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

NVP-HSP990, CAS 934343-74-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 105.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 343.00
100 mg	In stock	$ 571.00
1 mL * 10 mM (in DMSO)	In stock	$ 117.00

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Purity: 99.32%

Purity: 97.63%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NVP-HSP990 (HSP990) is an effective and specific HSP90α/β inhibitor (IC50: 0.6 /0.8 nM).
Targets&IC50	HSP90 β:0.8 nM, HSP90 α:0.6 nM
In vitro	NVP-HSP990 is based on a 2-amino-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one scaffold, which is structurally distinct from other known HSP90 inhibitors. NVP-HSP990 binds to the N-terminal ATP-binding domain of HSP90. NVP-HSP990 exhibits single digit nanomolar IC50 values on three of the HSP90 isoforms (HSP90α, HSP90β, and GRP94) and 320 nM IC50 value on the fourth (TRAP-1), with selectivity against unrelated enzymes, receptors, and kinases. NVP-HSP990 dissociates the HSP90-p23 complex, depleted client protein c-Met, and induced Hsp70 in c-Met amplified GTL-16 gastric tumor cells. NVP-HSP990 potently inhibites the growth of human cell lines and primary patient samples from a variety of tumor types. [1] NVP-HSP990 displays dose- and time-dependent effects on HSP90 client proteins. NVP-HSP990 inhibits Glioma tumor-initiating cells (GIC) proliferation in all GIC lines, with IC50 values ranging approximately between 10 and 500 nM. Olig2 is a functional marker associated with cell proliferation and response to NVP-HSP990, as NVP-HSP990 attenuated cell proliferation in Olig2-high GIC lines. In addition, NVP-HSP990 disrupted cell-cycle control mechanism by decreasing CDK2 and CDK4 and elevating apoptosis-related molecules. [2]
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. [1]
Kinase Assay	HSP90 binding, ATPase, and selectivity profiling assays: The potency of HSP90 inhibitors for HSP90α, HSP90β, and Grp94 is determined by AlphaScreen competition binding assays, and activity against TRAP-1 is assessed by an ATPase assay.
Cell Research	Dissociated GICs are plated at 10 cells/μL in 6-well plates and incubated with various concentrations of NVP-HSP990 for 7 days. Formed tumorspheres are dissociated into single cells and counted with hemocytometer using 0.2% Trypan blue exclusion. (Only for Reference)

Synonyms	HSP990
Molecular Weight	379.39
Formula	C20H18FN5O2
CAS No.	934343-74-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 70 mg/mL (184.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Menezes DL, et al. Mol Cancer Ther, 2012, 11(3), 730-739. 2. Fu J, et al. Cancer Res, 2013, 73(10), 3062-3074.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library HIF-1 Signaling Pathway Compound Library Fluorochemical Library Bioactive Compounds Library Max Anti-Aging Compound Library Apoptosis Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

NVP-HSP990 934343-74-5 Apoptosis Cytoskeletal Signaling Metabolism HSP Heat shock proteins NVP HSP990 NVP-HSP 990 Inhibitor HSP 990 HSP-990 inhibit NVPHSP990 HSP990 NVP-HSP-990 inhibitor

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