Ganetespib, HSP90 Inhibitor (TBI4474)

Description

Product Details

Formal Name: 3-(2,4-Dihydroxy-5-propan-2-ylphenyl)-4-(1-methylindol-5-yl)-1H-1,2,4-triazol-5-one

Alternate Names: STA-9090

Molecular Formula: C₂₀H₂₀N₄O₃

Formula Weight: 364.40

CAS Number: 888216-25-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

HSP90 Inhibitor

Functions

Ganetespib is an inhibitor of heat shock protein 90 (IC50 = 19 nM, canine C2 malignant mast cells; 4 nM, canine BR malignant mast cells) binding to the N-terminal ATP site. It displayed potent cytotoxicity against a panel of 57 transformed cell lines of both hematologic and solid tumors with IC50’s between 14 and 280 nM. Ganetespib enhanced T-cell-mediated killing of human melanoma cells and potentiated responses to anti-CTLA4 and anti-PD1 therapy via upregulation of interferon response genes. In multiple clinical trials for various cancers.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.