CCT251236 | HSF1 inhibitor

CCT251236 (1693731-40-06) 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:

  1. 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; Med. Chem., 60 180
  2. Fok et al. (2018), HSF-1: Essential for Myeloma Cell Survival and A Promising Therapeutic Target; Cancer Res., 124 2395
Weight 0.1 mg
Dimensions 0.1 × 0.1 × 0.1 cm
Size:

5 mg, 25 mg

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CAS:
1693731-40-6
Catalog Number:
10-4410
Activity:
Heat Shock Transcription Factor 1 stress pathway inhibitor
Chemical Names:
N-[5-(2,3-Dihydro-1,4-benzodioxine-6-carbonylamino)-2-methylphenyl]-2-(2-pyrrolidin-1-ylethoxy)quinoline-6-carboxamide
Molecular Weight:
552.63
Molecular Formula:
C32H32N4O5
Solubility:
Soluble in DMSO (5 mg/ml)
Physical Properties:
Off-white/beige solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

CCT251236 | HSF1 inhibitor

$90.00$325.00

CAS:
1693731-40-6
Catalog Number:
10-4410
Activity:
Heat Shock Transcription Factor 1 stress pathway inhibitor
Chemical Names:
N-[5-(2,3-Dihydro-1,4-benzodioxine-6-carbonylamino)-2-methylphenyl]-2-(2-pyrrolidin-1-ylethoxy)quinoline-6-carboxamide
Molecular Weight:
552.63
Molecular Formula:
C32H32N4O5
Solubility:
Soluble in DMSO (5 mg/ml)
Physical Properties:
Off-white/beige solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
Clear
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