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.

Size Price Stock Quantity  
USD 147 In stock
USD 477 In stock
USD 997 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • 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

Choose Selective HSP (e.g. HSP90) Inhibitors

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 NFXDeoNEgXSxdH;4bYNqfHliYYPzZZk> NF\zZnJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjB3ODDj[YxteyCrbjDwdoV{\W6lZTDv[kBJW0ZzIHvuc4NsKGSxd36geJJm[XSvZX70MEBKSzVyPUCuNFA2OiEQvF2= M1[zR|I3OTZ2MUi4
human A375 cells M{fpV2N6fG:2b4jpZ4l1gSCjc4PhfS=> MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIFjTSlEhc26xY3ug[I94diC2cnXheI1mdnRuIFnDOVA:OC5yME[g{txO M{TVWlI3OTZ2MUi4
human GTL16 cells NHza[ZZEgXSxdH;4bYNqfHliYYPzZZk> MVe3NkBp M2OwZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0doUuT2yxIHHzd4F6NCCLQ{WwQVAvODF2IN88US=> MkTZNlU{Pjh7OES=

... Click to View More Cell Line Experimental Data

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
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01064089 Terminated Advanced Solid Tumors Novartis Pharmaceuticals|Novartis February 2010 Phase 1
NCT00879905 Completed Advanced Solid Malignancies Novartis Pharmaceuticals|Novartis May 2009 Phase 1

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HSP (e.g. HSP90) Signaling Pathway Map

Related HSP (e.g. HSP90) Products

Tags: buy HSP990 (NVP-HSP990) | HSP990 (NVP-HSP990) supplier | purchase HSP990 (NVP-HSP990) | HSP990 (NVP-HSP990) cost | HSP990 (NVP-HSP990) manufacturer | order HSP990 (NVP-HSP990) | HSP990 (NVP-HSP990) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID