CCT251236 [1693731-40-6]
Referencia HY-101026-1mg
embalaje : 1mg
Marca : MedChemExpress
Contact local distributor :
Teléfono : +1 850 650 7790
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
CCT251236 Estructura química
No. CAS : 1693731-40-6
This product is a controlled substance and not for sale in your territory.
Based on 3 publication(s) in Google Scholar
| Descripciòn |
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] |
|
||||||||||||||||
| 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. Western Blot Analysis[1]
RT-PCR[1]
|
||||||||||||||||
| 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.
|
||||||||||||||||
| Peso molecular |
552.62 |
||||||||||||||||
| Fòrmula |
C32H32N4O5 |
||||||||||||||||
| No. CAS |
1693731-40-6 |
||||||||||||||||
| 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 |
||||||||||||||||
| Envío | Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
| Almacenamiento |
|
||||||||||||||||
| Solvente y solubilidad |
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
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
|
||||||||||||||||
| Pureza y Documentación | |||||||||||||||||
| Referencias |
|
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|
| DMSO | 1 mM | 1.8096 mL | 9.0478 mL | 18.0956 mL | 45.2390 mL |
| 5 mM | 0.3619 mL | 1.8096 mL | 3.6191 mL | 9.0478 mL | |
| 10 mM | 0.1810 mL | 0.9048 mL | 1.8096 mL | 4.5239 mL | |
| 15 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0159 mL | |
| 20 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2620 mL | |
| 25 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8096 mL | |
| 30 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5080 mL | |
| 40 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1310 mL | |
| 50 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 60 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 80 mM | 0.0226 mL | 0.1131 mL | 0.2262 mL | 0.5655 mL | |
| 100 mM | 0.0181 mL | 0.0905 mL | 0.1810 mL | 0.4524 mL |