N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)-2-(2-(pyrrolidin-1-yl)ethoxy)quinoline-6-carboxamide Chemical Properties

Boiling point:

628.7±55.0 °C(Predicted)

Density 

1.328±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO (5 mg/ml)

form 

solid

pka

12.18±0.70(Predicted)

color 

Off-white/beige

Stability:

Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)-2-(2-(pyrrolidin-1-yl)ethoxy)quinoline-6-carboxamide Usage And Synthesis

Description

CCT251236 (1693731-40-6) is 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).1 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.2

References

Cheeseman et al. (2017), Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen; J. Med. Chem., 60 180 Fok et al. (2018), HSF-1: Essential for Myeloma Cell Survival and A Promising Therapeutic Target; Cancer Res., 124 2395

N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)-2-(2-(pyrrolidin-1-yl)ethoxy)quinoline-6-carboxamide(1693731-40-6)Related Product Information

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