Art. -Nr.: HY-15190

NVP-HSP990

Name: NVP-HSP990
Brand: MedChemExpress
SKU: HY-15190
Price: 83.00 USD
Availability: InStock
Rating: 5 (4 reviews)

(Synonyms: HSP-990)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC₅₀ values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.

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Reinheit : 99.49%
CAS. Nr.: 934343-74-5
Formel: C₂₀H₁₈FN₅O₂
Molecular Weight:379.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

NVP-HSP990 Chemical Structure

CAS. Nr.: 934343-74-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC₅₀ values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.

IC₅₀ & Target

^[1]

HSP90α

0.6 nM (IC₅₀)

HSP90β

0.8 nM (IC₅₀)

GRP94

8.5 nM (IC₅₀)

TRAP1 ATPase

320 nM (IC₅₀)

Alle HSP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2058	IC₅₀	12.7 nM Compound: NVP-HSP990	Cytotoxicity against human A2058 cells in absence of HSF1 knock down treatment Cytotoxicity against human A2058 cells in absence of HSF1 knock down treatment	[PMID: 26164188]
A2058	IC₅₀	5.2 nM Compound: NVP-HSP990	Cytotoxicity against human A2058 cells in presence of HSF1 knock down treatment Cytotoxicity against human A2058 cells in presence of HSF1 knock down treatment	[PMID: 26164188]
A-375	IC₅₀	19 nM Compound: NVP-HSP990	Cytotoxicity against human A375 cells in absence of HSF1 knock down treatment Cytotoxicity against human A375 cells in absence of HSF1 knock down treatment	[PMID: 26164188]
A-375	IC₅₀	6 nM Compound: NVP-HSP990	Cytotoxicity against human A375 cells in presence of HSF1 knock down treatment Cytotoxicity against human A375 cells in presence of HSF1 knock down treatment	[PMID: 26164188]
GTL 16 cell line	EC₅₀	0.014 μM Compound: 9	Cytotoxicity against human GTL16 cells after 72 hrs by CellTitre-Glo assay Cytotoxicity against human GTL16 cells after 72 hrs by CellTitre-Glo assay	[PMID: 25368984]

In Vitro

NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC₅₀ values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively. NVP-HSP990 (10 μM) shows no affect the ATPase activity of topoisomerase II, a GHKL (Gyrase, Hsp90, Histidine Kinase, MutL) family ATPase, closely related to Hsp90. NVP-HSP990 also exerts efficient effects on c-Met, Hsp70, p-ERK and p-AKT in CTL-16 cells, with EC₅₀s of 37 ± 4, 20 ± 2, 11 ± 1, and 6 ± 1 nM, respectively. NVP-HSP990 suppresses the proliferation of BT474, A549, H1975 and MV4;11 cells, with GI₅₀s of 7 ± 2, 28 ± 5, 35 ± 4, and 4 ± 1 nM, respectively^[1]. NVP-HSP990 inhibits cellular proliferation of GTL-16, with an EC₅₀ of 14 nM^[2]. NVP-HSP990 (5-500 nM) inhibits the multiple myeloma cell lines, with IC₅₀s of 27-49 nM after treatment for 72 h. NVP-HSP990 induces apoptosis in multiple myeloma cell lines (0-100 nM), leads to cell cycle arrest in the G2/M phase (25-200 nM), and induces apoptosis via caspase-8 followed by caspase-3 activation (100 nM). NVP-HSP990 increases HSP70 expression and interacts with Akt and ERK signaling. Moreover, NVP-HSP990 (100 nM) in combination with melphalan, causes synergistic effects on growth inhibition in multiple myeloma cells and increases cleavage of caspase-3, caspase-8, and caspase-9 and activates caspase-2^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

NVP-HSP990 (2.5 to 5 mg/kg twice weekly, or 5 to 15 mg/kg weekly, p.o.) causes dose proportional antitumor efficacy, without obvious loss or overt signs of toxicity in a GTL-16 tumor bearing mice. NVP-HSP990 (5 or 10 mg/kg weekly, p.o.) also results in significant inhibition of tumor growth in BT-474 breast cancer model. NVP-HSP990 (5 mg/kg twice weekly or 15 mg/kg weekly, p.o.) inhibits the growth of tumor in the MV4;11 xenograft model. Furthermore, NVP-HSP990 (0.5 mg/kg every day, 14, 5 mg/kg twice weekly, or 15 mg/kg weekly, p.o.) displays antitumor efficacy in H1975 and A549 tumor models^[1]. NVP-HSP990 (5, 15 mg/kg, p.o.) shows prolonged suppression of c-Met levels with 30% and 50% reduction and exhibits antitumor activities in GTL-16 tumor xenograft^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 934343-74-5
Appearance Solid
Molecular Weight 379.39
Formel C₂₀H₁₈FN₅O₂
Color Off-white to yellow
SMILES

CC1=C2C(C[C@H](C3=C(C4=NC(OC)=CC=C4)C=C(F)C=C3)NC2=O)=NC(N)=N1
Synonyms

HSP-990
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Theranostics

Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]

2019 Aug 12;9(20):5769-5783. PMID: 31534518
Front Microbiol

Ketoconazole induces reversible antifungal drug tolerance mediated by trisomy of chromosome R in Candida albicans. [Abstract]

2024 Jul 30:15:1450557. PMID: 39139375
Viruses

Deep Transfer Learning Approach for Automatic Recognition of Drug Toxicity and Inhibition of SARS-CoV-2. [Abstract]

2021 Apr 2;13(4):610. PMID: 33918368
bioRxiv

2025 Oct 22.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 33 mg/mL (86.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6358 mL

13.1791 mL

26.3581 mL

5 mM

0.5272 mL

2.6358 mL

5.2716 mL

10 mM

0.2636 mL

1.3179 mL

2.6358 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

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

[2]. McBride CM, et al. Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990. J Med Chem. 2014 Nov 13;57(21):9124-9. [Content Brief]

[3]. Lamottke B, et al. The novel, orally bioavailable HSP90 inhibitor NVP-HSP990 induces cell cycle arrest and apoptosis in multiple myeloma cells and acts synergistically with melphalan by increased cleavage of caspases. Eur J Haematol. 2012 May;88(5):406-15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6358 mL	13.1791 mL	26.3581 mL	65.8953 mL
	5 mM	0.5272 mL	2.6358 mL	5.2716 mL	13.1791 mL
	10 mM	0.2636 mL	1.3179 mL	2.6358 mL	6.5895 mL
	15 mM	0.1757 mL	0.8786 mL	1.7572 mL	4.3930 mL
	20 mM	0.1318 mL	0.6590 mL	1.3179 mL	3.2948 mL
	25 mM	0.1054 mL	0.5272 mL	1.0543 mL	2.6358 mL
	30 mM	0.0879 mL	0.4393 mL	0.8786 mL	2.1965 mL
	40 mM	0.0659 mL	0.3295 mL	0.6590 mL	1.6474 mL
	50 mM	0.0527 mL	0.2636 mL	0.5272 mL	1.3179 mL
	60 mM	0.0439 mL	0.2197 mL	0.4393 mL	1.0983 mL
	80 mM	0.0329 mL	0.1647 mL	0.3295 mL	0.8237 mL

Bioz

Keywords

NVP-HSP990

4 Cited Publications

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NVP-HSP990

Publications Citing Use of MedChemExpress (MCE) NVP-HSP990

Alle HSP Isoform-spezifische Produkte anzeigen