PF15 TFA
Based on 1 Customer Validation
PF15 TFA is an orally active FLT3-ITD PROTAC degrader with a DC50 of 76.7 nM and an IC50 of 36 nM against FLT3-ITD. PF15 TFA induces FLT3-ITD protein degradation, thereby downregulating its phosphorylation level. PF15 TFA inhibits the proliferation of FLT3-ITD-positive cells and reduces the phosphorylation level of STAT5, a downstream molecule of FLT3-ITD. PF15 TFA exhibits efficacy in in vivo xenograft models of acute myeloid leukemia and prolongs survival. PF15 TFA can be used for the research of acute myeloid leukemia.
(Pink: FLT3 Target protein ligand; Blue: Cereblon ligand (HY-A0003); Black: linker).
For research use only. We do not sell to patients.
- Purity : 99.34%
- Formula: C46H50F3N13O8
- Molecular Weight:969.97
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
STAT5 |
In Vitro
PF15 (1-2000 nM; 1-24 h) induces proteasome-dependent degradation of FLT3 protein in BaF3-FLT3-ITD cells, with a DC50 of 76.7 nM, and prolonged incubation achieves complete degradation of the protein[1].
PF15 (10-1000 nM; 2 h) upregulates FLT3 mRNA levels in BaF3-FLT3-ITD cells at low concentrations (10 nM, 30 nM)[1].
PF15 (10-1000 nM; 6 h) downregulates the phosphorylation levels of FLT3 and STAT5 in BaF3-FLT3-ITD, BaF3-FLT3-ITD-D835V, and BaF3-FLT3-ITD-F691L cells at a concentration of 100 nM after 6 h of treatment, whereas a higher concentration is required for FLT3 degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PF15 (20-40 mg/kg; p.o.; twice daily; 12 days; i.p.; daily; 12 days) significantly extends survival in an AML in situ xenograft model, with the 20 mg/kg twice-daily p.o. dose increasing median survival from 11 days to 15 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Kinase activity and phosphorylation assays
- Western Blot
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Appearance Solid
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Molecular Weight 969.97
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Formula C46H50F3N13O8
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Color White to off-white
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SMILES
CC(C)(C1=CC(NC(NC2=CC=C(C=C2)C3=CN(C4=NC=NC(N)=C34)CCCCC5=CN(N=N5)CCCCC(NC6=C7CN(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=O)=NO1)C.O=C(O)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : ≥ 50 mg/mL (51.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (289 KB)
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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)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.0310 mL | 5.1548 mL | 10.3096 mL | 25.7740 mL |
| 5 mM | 0.2062 mL | 1.0310 mL | 2.0619 mL | 5.1548 mL | |
| 10 mM | 0.1031 mL | 0.5155 mL | 1.0310 mL | 2.5774 mL | |
| 15 mM | 0.0687 mL | 0.3437 mL | 0.6873 mL | 1.7183 mL | |
| 20 mM | 0.0515 mL | 0.2577 mL | 0.5155 mL | 1.2887 mL | |
| 25 mM | 0.0412 mL | 0.2062 mL | 0.4124 mL | 1.0310 mL | |
| 30 mM | 0.0344 mL | 0.1718 mL | 0.3437 mL | 0.8591 mL | |
| 40 mM | 0.0258 mL | 0.1289 mL | 0.2577 mL | 0.6443 mL | |
| 50 mM | 0.0206 mL | 0.1031 mL | 0.2062 mL | 0.5155 mL |
PF15 TFA Related Classifications
HY-143286A Related Classifications
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