产品
编 号：F202492
分子式：C32H32N4O5
分子量：552.62
分子式：C32H32N4O5
分子量：552.62
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1693731-40-6
产品详情
生物活性：
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
体内研究：
CCT251236 (oral adminstation; 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.CCT251236 (oral adminstation; 20 mg/kg; 33 days)has aclear 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.Animal Model:Athymic mice with SK-OV-3 cells
Dosage:20 mg/kg; 33 days
Administration:Oral adminstation
Result:Was efficacious in SK-OV-3 cell induced-tumor mice model.
体外研究：
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 with250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner.
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
体内研究：
CCT251236 (oral adminstation; 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.CCT251236 (oral adminstation; 20 mg/kg; 33 days)has aclear 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.Animal Model:Athymic mice with SK-OV-3 cells
Dosage:20 mg/kg; 33 days
Administration:Oral adminstation
Result:Was efficacious in SK-OV-3 cell induced-tumor mice model.
体外研究：
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 with250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner.
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