CCT251236 是通过热休克转录因子 1 (hsf1) 表型筛选得到的有口服活性的吡啶配体，抑制 HSF1 介导的 HSP72 诱导的 IC₅₀ 值为 19 nM。

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC 50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.

Solid

HSP72 19 nM (IC50, SK-OV-3 cells)

CCT251236 (0-100 nM; 24hours) displays a 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.
CCT251236 (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.
CCT251236 (0-100 nM; 24 hours), pre-treated with 250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner.
has not independently confirmed the accuracy of these methods. They are for reference only.

CCT251236 (oral adminstation; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free C av  value of 2.0 nM and 1.2 nM, respectively.
CCT251236 (oral adminstation; 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 decreases 64% when compares to control group. In addition, the compound’s basicity and high volume of distribution shows in tumor withtumor concentrations of CCT251236 as high as 940 nM.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 150 mg/mL (271.43 mM)配制储备液