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CCT251236

  Cat. No.:  DC10498   Featured
Chemical Structure
1693731-40-6
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1693731-40-6
Chemical Name: CCT251236
Synonyms: CCT251236
SMILES: CC1=CC=C(NC(C2=CC(OCCO3)=C3C=C2)=O)C=C1NC(C4=CC(C=CC(OCCN5CCCC5)=N6)=C6C=C4)=O
Formula: C32H32N4O5
M.Wt: 552.620287895203
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
In Vivo: CCT251236 possesses low total blood clearance (10% hepatic blood flow) and moderate oral bioavailability, with a half-life sufficient to allow once-a-day dosing. Clear therapeutic efficacy is observed with CCT251236, with a tumor growth inhibition of 70% based on final tumor volumes[1].
In Vitro: CCT251236 displays the desired balance of in vitro properties, while maintaining excellent cellular activity with an IC50 of 19 nM. The free GI50 in SK-OV-3 cells is 1.1 nM. Western blotting confirms that CCT251236 blocks the HSF1-mediated induction of both HSP72 and HSP27 as representative heat shock proteins, following treatment with the HSP90 inhibitor 17AAG. Also, qPCR analysis demonstrates that CCT251236 inhibits the induction of HSP72 at the mRNA level, clearly blocking the induction of HSPA1A gene expression with an IC50 of 40 nM[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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