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CCT251236

Catalog No. T14905   CAS 1693731-40-6

CCT251236 is an orally available Pirin ligand obtained from a heat shock transcription factor 1 (hsf1) phenotypic screen. It inhibits HSF1-mediated HSP72 induction (IC50: 19 nM).

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CCT251236 Chemical Structure
CCT251236, CAS 1693731-40-6
Pack Size Availability Price/USD Quantity
50 mg 6-8 weeks $ 737.00
100 mg 6-8 weeks $ 1,170.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CCT251236 is an orally available Pirin ligand obtained from a heat shock transcription factor 1 (hsf1) phenotypic screen. It inhibits HSF1-mediated HSP72 induction (IC50: 19 nM).
Targets&IC50 SK-OV-3 cells:, HSP72:19 nM
In vitro CCT367766 (0-100 nM; 24 hours) blocks 17-AAG induced he HSF1-mediated heat-shock proteins, HSP72, and HSP27 expression as a concentration manner in SK-OV-3 cells. CCT367766 blocks the induction of HSPA1A mRNA by 17-AAG in a dose-dependent manner. CCT367766 (0-100 nM; 24hours) displays the desired balance of in vitro properties while maintaining excellent cellular activity with a pIC50=7.73 ± 0.07 (IC50: 19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI50?is 1.1 nM in SK-OV-3 cells that calculated from the free fraction in the cell assay. CCT367766 (0-100 nM; 24 hours) pre-treated with 250 nM 17-AAG for 6h.
In vivo CCT367766 (p.o.; 20 mg/kg; 33 days) has a clear therapeutic efficacy in mice with a tumor growth inhibition (%TGI) of 70% based on final tumor volumes. After 33 days, the mean tumor weights decrease 64% when compares to the control group. In addition, the compound's basicity and the high volume of the distribution shown in tumors with tumor concentrations of?CCT367766?as high as 940 nM. CCT367766 (p.o.; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free?Cav0–24h?value of 2.0 nM and 1.2 nM, respectively [2].
Molecular Weight 552.62
Formula C32H32N4O5
CAS No. 1693731-40-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (271.43 mM)

TargetMolReferences and Literature

1. Cheeseman MD, et al. Discovery of a Chemical Probe Bisamide (CCT251236): An OrallyBioavailable Efficacious Pirin Ligand from a Heat ShockTranscription Factor 1 (HSF1) Phenotypic Screen. J Med Chem. 2017 Jan 12;60(1):180-201.

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Keywords

CCT251236 1693731-40-6 Cytoskeletal Signaling Metabolism HSP CCT-251236 CCT 251236 inhibitor inhibit

 

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