Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare
 
> CCT251236 [1693731-40-6]

CCT251236 [1693731-40-6]

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Cat# HY-101026-1mg

Size : 1mg

Marca : MedChemExpress


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.

IC50 & Target[1]

HSP72

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

Cellular Effect
Cell Line Type Value Description References
SK-OV-3 GI50
1.1 nM
Compound: 26
Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay
Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay
[PMID: 28004573]
SK-OV-3 GI50
2.2 nM
Compound: 26
Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay
Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay
[PMID: 28004573]
SK-OV-3 GI50
2.2 nM
Compound: 1; CCT251236
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 96 hrs by resazurin dye based celltiter-blue viability assay
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 96 hrs by resazurin dye based celltiter-blue viability assay
[PMID: 37017629]
WM 266-4 GI50
12 nM
Compound: 26
Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay
Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay
[PMID: 28004573]
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 (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[1].
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[1].
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CCT251236 Related Antibodies

Western Blot Analysis[1]

Cell 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-PCR[1]

Cell 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 Cav0-24h value of 2.0 nM and 1.2 nM, respectively[2].
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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic mice with SK-OV-3 cells[2]
Dosage: 20 mg/kg; 33 days
Administration: Oral adminstation
Result: Was efficacious in SK-OV-3 cell induced-tumor mice model.
Masse moléculaire

552.62

Formule

C32H32N4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=C(NC(C2=CC(OCCO3)=C3C=C2)=O)C=C1NC(C4=CC(C=CC(OCCN5CCCC5)=N6)=C6C=C4)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (180.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8096 mL 9.0478 mL 18.0956 mL
5 mM 0.3619 mL 1.8096 mL 3.6191 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (4.52 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
Références

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