HSP990 (NVP-HSP990)

Catalog No.S7097

HSP990 (NVP-HSP990) Chemical Structure

Molecular Weight(MW): 379.39

NVP-HSP990 (HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM.

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Cited by 2 Publications

2 Customer Reviews

  • Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.

    Cancer Sci, 2018, 109(2):373-383. HSP990 (NVP-HSP990) purchased from Selleck.

    Time killing curves of C. albicans 103 treated with HSP990 and FLC. FLC-resistant C. albicans 103 were treated with FLC (4 μg/ml), HSP990 (8 μg/ml and FLC+HSP990 (4+8) μg/ml by using initial inoculums of 105 CFU/ml. Aliquots were obtained at the indicated time points and serially dilutions were spreaded on SDA agar plates. Colony counts were determined after 48 h incubation.

    Am J Transl Res,2015, 7(12):2589-602.. HSP990 (NVP-HSP990) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description NVP-HSP990 (HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM.
Features NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.
Targets
HSP90α [1]
(Cell-free assay)		 HSP90β [1]
(Cell-free assay)
0.6 nM 0.8 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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2058 cells MnL4R5l1d3SxeHnjbZR6KGG|c3H5 NIPwfXJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjB3ODDj[YxteyCrbjDwdoV{\W6lZTDv[kBJW0ZzIHvuc4NsKGSxd36geJJm[XSvZX70MEBKSzVyPUCuNFA2OiEQvF2= NGrhZnozPjF4NEG4PC=>
human A375 cells NV7ybW9zS3m2b4TvfIlkcXS7IHHzd4F6 NVL2[ZY5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTN5NTDj[YxteyCrbjDwdoV{\W6lZTDv[kBJW0ZzIHvuc4NsKGSxd36geJJm[XSvZX70MEBKSzVyPUCuNFA3KM7:TR?= NFHLc5UzPjF4NEG4PC=>
human GTL16 cells NWewRZNuS3m2b4TvfIlkcXS7IHHzd4F6 MWW3NkBp NUX5eIE6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT1SOMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRz\S2JbH:gZZN{[XluIFnDOVA:OC5yMUSg{txO MXqyOVM3QDl6NB?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
HSP90 / HSP70 ; 

PubMed: 24100469     


HSP990 for 2 and 24 h. Subsequently the expression of HSP90 and HSP70 was evaluated by western blot analysis. A representative blot of 3 independently performed experiments is shown

EGFR / ErbB2 / ErbB3 / IGF-1R ; 

PubMed: 24100469     


Effect of HSP90 inhibition on RTK expression in neuroendocrine BON1 tumor cells. BON1, NCI-H727 and GOT1 cells were treated with increasing concentrations (1-100 nM) of the HSP90 inhibitor HSP990 (right panel) for 24 h. Subsequently the expression of EGFR, ErbB2, ErbB3 and IGFIR was evaluated by western blot analysis. A representative blot out of 3 independently performed experiments is shown.

p-Akt / Akt / p-ERK / ERK / pp70S6K / p70S6K / p4EBP1 / 4EBP1 ; 

PubMed: 24100469     


Effect of HSP90 inhibition on downstream signaling. BON1, NCI-H727 and GOT1 cells were treated with increasing concentrations (1–100 nM) of the HSP90 inhibitor AUY922 (left panel) or HSP990 (right panel) for 24 h. Subsequently, the expression of pErk1/2, Erk1/2, pAkt, Akt, pp70S6K, p70S6K, p4EBP1 and 4EBP1 was evaluated by western blot analysis. A representative blot out of 3 independently performed experiments is shown.

24100469
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]

Protocol

Kinase Assay:

[1]
+ Expand

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:

[2]
+ Expand
  • Cell lines: GICs
  • Concentrations: ~1 μM
  • Incubation Time: 7 days
  • Method:

    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)
Animal Research:

[1]
+ Expand
  • Animal Models: GTL-16, NCI-H1975, BT474, and MV4;11 tumor xenografted nude and SCID mice models
  • Formulation: 100% polyethylene glycol (PEG400)
  • Dosages: 15 mg/kg
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (197.68 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 379.39
Formula

C20H18FN5O2
CAS No. 934343-74-5
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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HSP (e.g. HSP90) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID