CCT251236 - 10mM in DMSO , CAS No.1693731-40-6

CAS: 1693731-40-6 Cat. No.: C655419 Summenformel: C₃₂H₃₂N₄O₅ Molekulargewicht: 552.62 EG-Nummer: 849-595-6 PubChem CID: 117996749

QUALITÄT & REINHEIT Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

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.

In Vitro

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 (IC 50 =19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: SK-OV-3 cells Concentration: 0 nM; 10 nM; 100 nM Incubation Time: 24 hours Result: Inhibited HSP72 and HSP27 expression at the dose of 10 nM. RT-PCRCell Line: SK-OV-3 cells Concentration: 0 nM; 10 nM; 100 nM and 1000 nM Incubation Time: 24 hours Result: Decreased HSPA1A mRNA level.

In Vivo

CCT251236 (oral adminstation; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free C av 0-24h 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic mice with SK-OV-3 cellsDosage: 20 mg/kg; 33 days Administration: Oral adminstation Result: Was efficacious in SK-OV-3 cell induced-tumor mice model.

IC50& Target:HSP72 19 nM (IC 50 , SK-OV-3 cells)

Spezifikationen

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

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.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Namen und Kennungen

Isomere SMILES

CC1=C(C=C(C=C1)NC(=O)C2=CC3=C(C=C2)OCCO3)NC(=O)C4=CC5=C(C=C4)N=C(C=C5)OCCN6CCCC6

Alternative CAS-Nummer

1693731-40-6

PubChem CID

117996749

MeSH-Eintrag

CCT251236

Molekulargewicht

552.62

Zugehörige Ziele (menschlich)

HSF1 Tchem Heat shock factor protein 1 (4 Activities)

Discover Target: HSF1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIR Tchem Pirin (5 Activities)

Discover Target: PIR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1693731-40-6, the molecular formula is C32H32N4O5, and the molecular weight is 552.62 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.