NVP-HSP990

SKU: orb1301057

Description

NVP-HSP990 (HSP990) is a potent and selective HSP90α/β inhibitor with IC50 values of 0.6 nM and 0.8 nM, respectively. It is widely used in cancer research to study oncogenic client protein degradation and has demonstrated antitumor efficacy in both cellular assays and in vivo xenograft models.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	934343-74-5
MW	379.39
Purity	98.03%
Formula	C₂₀H₁₈FN₅O₂
SMILES	COC1=CC=CC(=N1)C1=C(C=CC(F)=C1)C1CC2=C(C(C)=NC(N)=N2)C(=O)N1
Target	Apoptosis,HSP
Solubility	DMSO:70 mg/mL (184.51 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.27 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	TRAP1:320 nM\|HSP90 α:0.6 nM\|GRP94:8.5 nM\|HSP90 β:0.8 nM
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. Read more...
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. 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. Read more...
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) Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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NVP HSP990, NVP-HSP 990, NVPHSP990, NVP-HSP990, NVP-HSP-990, inhibit, Inhibitor, Heat shock proteins, HSP90α, HSP90β, HSP990, HSP-990, HSP 990, HSP, Apoptosis

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Compound Identifiers

PubChem CID

16226182 ↗

Key Properties

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No computed properties available.

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NVP-HSP990 (orb1301057)

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Purity:	>98% (HPLC)
CAS Number:	934343-74-5
MW:	379.39
Formula:	C₂₀H₁₈FN₅O₂

NVP-HSP990

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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