1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. VER-82576

VER-82576 (Synonyms: NVP-BEP800)

Cat. No.: HY-10942 Purity: 99.56%
Handling Instructions

VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.

For research use only. We do not sell to patients.

VER-82576 Chemical Structure

VER-82576 Chemical Structure

CAS No. : 847559-80-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1176 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All HSP Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.

IC50 & Target

HSP90β

58 nM (IC50)

GRP94

4.1 μM (IC50)

TRAP-1

5.5 μM (IC50)

In Vitro

VER-82576 (NVP-BEP800) is a potent and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β and is >70-fold selective against Grp94 and Trap-1, with IC50s of 4.1 ± 1.1 and 5.5 ± 0.48 μM. VER-82576 potently inhibits the proliferation of tumor cells, with GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, with an average GI50 of 245 nM. VER-82576 (250-1250 nM) depletes client proteins in human cancer cell lines in vitro[1]. VER-82576 (NVP-BEP800; 200 nM) shows no significant effect on the ionizing radiation (IR) dose-response curves of A549 cells, and is less toxic to SNB19 cells. VER-82576 in combination with IR results in more severe DNA damage in both A549 and SNB19 cell lines than each treatment alone and also protracts the kinetics of DNA damage repair in SNB19 cells[2]. VER-82576 (NVP-BEP800; 0.05, 0.1 or 0.2 μM) dose-dependently decreases the viability and induces apoptosis of glioblastoma cells. VER-82576 (0.2 μM) suppresses the expression of IKKβ protein but does not alter the levels of IKKβ mRNA in T98G cells. VER-82576 (0.2 μM) suppresses the expression of heat shock protein 70[3].

In Vivo

VER-82576 (NVP-BEP800; 15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice[1].

Molecular Weight

480.41

Formula

C₂₁H₂₃Cl₂N₅O₂S

CAS No.

847559-80-2

SMILES

O=C(C1=CC2=C(N=C(N=C2S1)N)C3=CC(OCCN4CCCC4)=C(C=C3Cl)Cl)NCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.2 mg/mL (12.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0816 mL 10.4078 mL 20.8156 mL
5 mM 0.4163 mL 2.0816 mL 4.1631 mL
10 mM 0.2082 mL 1.0408 mL 2.0816 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[3]

Prior to treatments, the cells are placed into 6-well plates in medium at a density of 1 × 105 cells/well, three wells per treatment group and cultured for 24 h. The cells are divided into treatment groups and treated accordingly for 40 h: vehicle control (DMSO, 0.016%, v/v), VER-82576 (0.05, 0.1 or 0.2 μM), irradiation (10 Gy), or VER-82576 (0.05, 0.1 or 0.2 μM) in combination with irradiation (10 Gy). Upon completion of the treatment, all cells are incubated with 0.5 mg/ml MTT for 3 h. The relative viability of the treated cells to the untreated control cells is measured. The absorbance is measured at 490 nm on a microplate reader[3].

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

Animal Administration
[1]

The estrogen receptor (ER)-positive, ErbB2-overexpressing cell line BT-474 is grown in DMEM high glucose (4.5 g/L) supplemented with 10% FCS, 200 mM l-glutamine, and 1% sodium pyruvate (BioConcept). Two or 3 d before cell inoculation, each mouse is s.c. implanted on the upper dorsal side with a 17β-estradiol pellet (25 μg/d; 90-d release) using a trocar needle. BT-474 cells (5 × 106) are injected in 200 μL Matrigel/HBSS (1:1 volume) s.c. in the right flank. The A375 cell line expresses mutant B-Raf (V600E). The cells are grown in RPMI 1640 supplemented with 10% FCS and 200 mM l-glutamine. To establish tumors, 5 × 106 A375 cells are injected s.c. in 200 μL PBS in the right flank. The animals are kept under optimized hygienic conditions with a 12-h dark, 12-h light cycle. The animals are fed food and water ad libitum. Tumor growth and body weights are monitored at regular intervals. The xenograft tumor sizes are measured manually with calipers, and the tumor volume is estimated using the following formula: (W × L × H × π/6), where width (W), length (L), and height (H) are the three largest diameters. Treatment with VER-82576 is initiated when the average tumor volume reaches 100 to 300 mm3[1].

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

References

Purity: 99.56%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

VER-82576NVP-BEP800VER82576VER 82576HSPHeat shock proteinsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
VER-82576
Cat. No.:
HY-10942
Quantity:
MCE Japan Authorized Agent: