NVP-BEP800

Catalog No.S1498 Synonyms: VER82576

NVP-BEP800 Chemical Structure

Molecular Weight(MW): 480.41

NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1.

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2 Customer Reviews

  • Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800).

    Cancer Cell 2012 20(3), 400-13. NVP-BEP800 purchased from Selleck.

    Western blots show the molecular signature of HSP90 inhibition by NVP-BEP800 (ie, induction of HSP72 and depletion of client proteins such as ERBB2, CRAF and CDK4) in BT474 breast cancer cell line. GAPDH was used as loading control.

     

     

    Dr. Swee Sharp and Professor Paul Workman from Cancer Research UK. NVP-BEP800 purchased from Selleck.

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Notes:

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Biological Activity

Description NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1.
Targets
HSP90β [1]
58 nM
In vitro

NVP-BEP800 is an ATP-competitive inhibitor of Hsp90β with an IC50 of 58 nM, exhibiting >70-fold selectivity against Hsp90 family members Grp94 and Trap-1 with IC50 values of 4.1 μM and 5.5 μM, respectively. NVP-BEP800 displays no inhibitory activity against the closely related GHKL ATPase, topoisomerase II, and the structurally unrelated ATPase, Hsp70 at the concentration of 10 μM. NVP-BEP800 potently inhibits the proliferation of various tumor cell lines with GI50 values ranging from 38 nM in A375 to 1.05 μM in PC3, and primary human tumors with the mean IC50 of 0.75 μM and IC70 of 1.8 μM. NVP-BEP800 treatment at the concentration of five times the GI50 increases the percentage of G2-M phase in A2058 and A549 cells and sub-G1 phase in BT-474, HCT116, A2058 and A549 cells by 29.5%, 33.6%, 42.7%, 12.1%, 5.9% and 7.1%, respectively. NVP-BEP800 treatment causes Akt and ErbB2 dephosphorylation, ErbB2 degradation, and Hsp70 induction in a concentration-dependent manner in BT-474 cells with IC50 values of 218 nM, 39.5 nM, 137 nM and 207 nM, respectively. [1]

In vivo Oral administration of NVP-BEP800 at 15 or 30 mg/kg/day for 15 days causes a dose-dependent reduction in B-Raf and Akt phosphorylation levels, and displays significant dose-dependent antitumor efficacy in the A375 melanoma xenograft model with the T/C values of 53% and 6% at the dose of 15 and 30 mg/kg/day, respectively, suggesting almost complete tumor inhibition at 30 mg/kg/day. Administration of NVP-BEP800 induces dose-dependent increase of Hsp90-p23 complex dissociation and reductions in the levels of steady-state ErbB2, phospho-Akt and phospho-S6, in BT-474 breast cancer xenografts, and exhibits significant antitumor activity with 38% tumor regression at dose of 30 mg/kg/day and a T/C of 36% at dose of 15 mg/kg/day. [1]

Protocol

Kinase Assay
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Competitive binding fluorescent polarization assay:

Recombinant Hsp90β, TAMRA-radicicol, or various concentrations of NVP-BEP800 is added in assay buffer (50 mM TRIS pH 7.4, 5 mM MgCl2, 150 mM KCl, and 0.1% CHAPS), mixed, and incubated at room temperature for 30 to 45 minutes prior to reading. The 2D-FIDA-based HTS assay based on confocal technologies monitors the decreased fluorescence polarization on displacement of the high affinity ligand TAMRA-radicicol from Hsp90β by NVP-BEP800. The concentration of NVP-BEP800 which inhibits Hsp90β by 50% is determined from the competition curve.
Cell Research
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  • Cell lines: A375, PC3, A2058, A549, HCT116, BT-474, SKBr3, MCF-7, MDAMB-157, MDA-MB-231, MDA-MB-468, and BT20
  • Concentrations: Dissolved in DMSO as a 10 mM stock solution, final concentrations ~1 mM
  • Incubation Time: 24 hours
  • Method: Cells are exposed to NVP-BEP800 for 24 hours. Cell proliferation is determined using either sulforhodamine B for adherent cells or MTS assay for suspension cells or those showing low adherence. Cell death is determined using a ToxiLight nondestructive cytotoxicity bioassay kit. Cell cycle progression is determined by RNase A/propidium iodide staining following fixation in 70% ethanol. Caspase-3/7 activity is determined using a homogeneous caspase activity kit.
    (Only for Reference)
Animal Research
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  • Animal Models: Female Harlan HsdNpa: Athymic Nude-nu mice injected s.c. with BT-474 or A375 cells
  • Formulation: Formulated as a suspension in 0.5% methyl cellulose
  • Dosages: ~50 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 15 mg/mL (31.22 mM)
DMSO <1 mg/mL
Water <1 mg/mL
In vivo 0.5% methylcellulose 5 mg/mL

* 1 mg/ml means slightly soluble or 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 480.41
Formula

C21H23Cl2N5O2S

CAS No. 847559-80-2
Storage powder
in solvent
Synonyms VER82576

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID