CCT251236, HSF1 inhibitor (TBI4410)

Description

Product Details

Formal Name: N-[5-(2,3-Dihydro-1,4-benzodioxine-6-carbonylamino)-2-methylphenyl]-2-(2-pyrrolidin-1-ylethoxy)quinoline-6-carboxamide

Molecular Formula: C₃₂H₃₂N₄O₅

Formula Weight: 552.60

CAS Number: 1693731-40-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 5 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

HSF1 inhibitor

Functions

An inhibitor of the Heat Shock Transcription Factor 1 (HSF1) stress pathway (IC50 = 19 nM Inhibition HSF-1 mediated HSP72 induction, IC50 = 40 nM HSPA1A induction). It displayed efficacy in a human ovarian carcinoma xenograft mouse model (SK-OV 3 cells) and inhibited migration of WM266.4 melanoma cells @ 100 nM. CCT251236 showed high affinity for the protein pirin (Ki = 28 nM), but this target was not shown conclusively to be the cause of the anticancer activity. It also showed efficacy in vitro against primary patient-derived myeloma cells and H929 human myeloma xenograft models.

Application Procedures

First dissolved in DMSO (up to 5 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.