PF-06952229
Based on 4 publication(s) in Google Scholar
PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.80%
- CAS No.: 1801333-55-0
- Formule: C23H24ClFN4O3
- Masse moléculaire:458.91
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PF-06952229
More
Customer Validation & Images
-
WB
-
RT-PCR
-
Cell Migration/Invasion Assay
Activité biologique
Description
IC50 & Target
IC50: transforming growth factor-beta receptor 1 (TGFbR1)[1]
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MCF-7 ER+ HER2-xenograft breast cancer tumor model[1]
-
Dosage:30 mg/kg
-
Administration:Oral gavage; twice daily; 44 days
-
Result:Resulted in an increase in tumor growth inhibition when combined with Palbociclib.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1801333-55-0
-
Appearance Solid
-
Masse moléculaire 458.91
-
Formule C23H24ClFN4O3
-
Color White to off-white
-
SMILES
O=C(NC(CO)CO)C1=CN=CC=C1NC2=CC(C3=CC(Cl)=CC=C3F)=NC=C2C(C)C
-
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
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Cell Discov
Single-cell transcriptome reveals cellular hierarchies and guides p-EMT-targeted trial in skull base chordoma. [Abstract]2022 Sep 20;8(1):94. PMID: 36127333
PF-06952229 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI protein levels in the UM‑Chor1 cell line.
PF-06952229 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI mRNA levels in the UM‑Chor1 cell line.
PF-06952229 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h attenuated the invasiveness of UM‑Chor1 cells.
-
Cell Commun Signal
Prkci promotes colorectal cancer metastasis by phosphorylating and stabilizing Tgfbr1 to activate TGF-β signaling. [Abstract]2025 May 17;23(1):230. PMID: 40382656 -
Commun Biol
Wnt11 mediates fibroblast-smooth muscle cell interaction to promote neurogenic bladder fibrosis in rats. [Abstract]2026 Feb 9;9(1):194. PMID: 41663583 -
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (108.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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:
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.45 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
-
Fiche technique (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instruction de manipulation (2659 KB)
Références
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 | 2.1791 mL | 10.8954 mL | 21.7908 mL | 54.4769 mL |
| 5 mM | 0.4358 mL | 2.1791 mL | 4.3582 mL | 10.8954 mL | |
| 10 mM | 0.2179 mL | 1.0895 mL | 2.1791 mL | 5.4477 mL | |
| 15 mM | 0.1453 mL | 0.7264 mL | 1.4527 mL | 3.6318 mL | |
| 20 mM | 0.1090 mL | 0.5448 mL | 1.0895 mL | 2.7238 mL | |
| 25 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1791 mL | |
| 30 mM | 0.0726 mL | 0.3632 mL | 0.7264 mL | 1.8159 mL | |
| 40 mM | 0.0545 mL | 0.2724 mL | 0.5448 mL | 1.3619 mL | |
| 50 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 60 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9079 mL | |
| 80 mM | 0.0272 mL | 0.1362 mL | 0.2724 mL | 0.6810 mL | |
| 100 mM | 0.0218 mL | 0.1090 mL | 0.2179 mL | 0.5448 mL |
PF-06952229 Related Classifications
HY-136244 Related Classifications
Powered by Bioz