VER-82576

SKU: orb1306450

Description

VER-82576

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 847559-80-2
• MW: 480.41
• Purity: 98.87%
• Formula: C₂₁H₂₃Cl₂N₅O₂S
• SMILES: CCNC(=O)c1cc2c(nc(N)nc2s1)-c1cc(OCCN2CCCC2)c(Cl)cc1Cl
• Target: HSP
• Solubility: DMSO:1 mg/mL (2.08 mM)

Bioactivity

• Target IC50:
  HSP90 β:58 nM|GRP94:4.1 μM|TRAP1:5.5 μM
• In Vivo:
  NVP-BEP800 effectively inhibited the proliferation of various tumor cell lines including A375 cells (GI50: 38 nM) and PC3 cells (GI50: 1.05 μM). In A2058 and A549 cells, NVP-BEP800 (5-fold of GI50) increased the G2-M phase percentage. In BT-474 cells, NVP-BEP800 induced Akt and ErbB2 dephosphorylation, ErbB2 degradation, and Hsp70 induction in a concentration-dependent manner (IC50: 218/39.5/137/207 nM).At a concentration of 10 μM of Hsp70, the effects of NVP-BEP800 on the closely related GHKL ATPase, topoisomerase II, and structurally unrelated ATPases were observed. II and structurally unrelated ATPases were not significantly inhibited.
• In Vitro:
  In the A375 malignant melanoma transplantation tumor model, NVP-BEP800 (15 or 30 mg/kg/day, p.o.) treatment for 15 days dose-dependently decreased the levels of B-Raf and Akt phosphorylation and showed anticancer activity, with T/C values of 53% and 6% with NVP-BEP800 (15 and 30 mg/kg/day) treatment and almost total tumor inhibition with 30 mg/kg/day. 30 mg/kg inhibited almost all tumors. In BT-474 breast cancer transplantation tumors, NVP-BEP800 treatment increased the dissociation of Hsp90-p23 complex and decreased the levels of stable ErbB2, p-Akt and p-S6 in a dose-dependent manner, and NVP-BEP800 (30 mg/kg/day) treatment resulted in 38% tumor regression. Treatment with 15 mg/kg/day resulted in a T/C of 36%.
• Cell Research:
  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)

Storage & Handling

• Storage: 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

inhibit, NVP-BEP 800, NVP-BEP800, NVP-BEP-800, HSP90β, HSP, Inhibitor, Heat shock proteins, VER 82576, VER82576, VER-82576

Compound Identifiers

PubChem CID

25210273