PF-06273340
Based on 1 Customer Validation
PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.8%
- No. CAS: 1402438-74-7
- Fòrmula: C23H22ClN7O3
- Peso molecular:479.92
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Heterocyclic Compound Library
HY-L138
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Pain-Related Compound Library
HY-L139
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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Anti-Brain Cancer Compound Library
HY-L188
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
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Kinase Inhibitor Library
HY-L009
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Neuronal Signaling Compound Library
HY-L013
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Protein Tyrosine Kinase Compound Library
HY-L016
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Clinical Compound Library
HY-L026
Actividad biológica
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TrkC 3 nM (IC50) |
TrkB 4 nM (IC50) |
TrkA 6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>300 μM
Compound: 14; PF-06273340
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Toxicity in human HepG2 cells
Toxicity in human HepG2 cells
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[PMID: 27766865] |
PF-06273340 potently inhibits TrkA, TrkB, and TrkC kinases with IC50 values of 6 nM, 4 nM, and 3 nM, respectively[1].
PF-06273340 exhibits low metabolic turnover in human liver microsomes, with a rate of <8.0 μL/min/mg protein[1].
PF-06273340 is a good substrate for P-glycoprotein, as demonstrated by an efflux ratio of 35.7 in the MDCK-MDR1 assay[1].
PF-06273340 is a substrate for BCRP, as demonstrated by an efflux ratio of 4.0[1].
PF-06273340 (1 μM) is highly kinase-selective, potently inhibiting only MUSK (IC50 = 53 nM), FLT-3 (IC50 = 395 nM), IRAK1 (IC50 = 2.5 μM), MKK (90% at 1 μM), and DDR1 (60% at 1 μM) among 309 tested kinases[1].
PF-06273340 has no measurable activity at the hERG channel, with an IC50 >30.0 μM[1].
PF-06273340 exhibits minimal cytotoxicity in THLE cells (IC50 >42 μM) and HepG2 cells (IC50 >300 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1402438-74-7
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Appearance Solid
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Peso molecular 479.92
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Fòrmula C23H22ClN7O3
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC(C(C2=CN(C(C)(C)CO)C3=NC(N)=NC=C32)=O)=CN=C1)CC4=NC=C(Cl)C=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 20 mg/mL (41.67 mM; Need ultrasonic and warming; 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, 6 months; -20°C, 1 month. 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. 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)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
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, 6 months; -20°C, 1 month. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0837 mL | 10.4184 mL | 20.8368 mL | 52.0920 mL |
| 5 mM | 0.4167 mL | 2.0837 mL | 4.1674 mL | 10.4184 mL | |
| 10 mM | 0.2084 mL | 1.0418 mL | 2.0837 mL | 5.2092 mL | |
| 15 mM | 0.1389 mL | 0.6946 mL | 1.3891 mL | 3.4728 mL | |
| 20 mM | 0.1042 mL | 0.5209 mL | 1.0418 mL | 2.6046 mL | |
| 25 mM | 0.0833 mL | 0.4167 mL | 0.8335 mL | 2.0837 mL | |
| 30 mM | 0.0695 mL | 0.3473 mL | 0.6946 mL | 1.7364 mL | |
| 40 mM | 0.0521 mL | 0.2605 mL | 0.5209 mL | 1.3023 mL |
PF-06273340 Related Classifications
HY-122616 Related Classifications
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