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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, CAS 1693731-40-6

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Purity: 98%

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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	HSP72:19 nM, SK-OV-3 cells:
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 2 years

Solubility Information

DMSO: 150 mg/mL (271.43 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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 Inhibitor inhibitor inhibit

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