SOS1-IN-14
Based on 1 Customer Validation
SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.60%
- No. CAS: 2793405-20-4
- Fòrmula: C29H29F3N6O2
- Peso molecular:550.57
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Almacenamiento:Powder -20°C, 3 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
Actividad biológica
Descripciòn
IC50 & Target
IC50: 3.9 nM (SOS1)[1]
In Vitro
SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50 of 21 nM[1].
SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC50s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles[1].
Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs[1].
| ICR Mice | Sprague–Dawley Rats | Beagle Dogs | |||
| Administration | p.o., 50 mg/kg | i.v., 2 mg/kg | p.o., 10 mg/kg | i.v., 2 mg/kg | p.o., 20 mg/kg |
| Tmax (h) | 0.5 | 0.08 | 3 | 0.08 | 2 |
| T1/2 (h) | 4.61 | 1.17 | 2.32 | 3.83 | 6.68 |
| Cmax (μg/mL) | 2670 | 1261 | 265 | 568 | 1840 |
| AUC0-24 (ng/mL·h) | 32300 | 970 | 1683 | 2962 | 25725 |
| CL (mL/min/kg) | / | 2068 | / | 11.3 | / |
| Vss (L/kg) | / | 2126 | / | 3.88 | / |
| F (%) | / | / | 34.5 | / | 86.8 |
| Kel (h-1) | 0.265 | / | / | / | / |
| MRT (h) | 4.67 | / | / | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2793405-20-4
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Appearance Solid
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Peso molecular 550.57
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Fòrmula C29H29F3N6O2
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Color Light yellow to light brown
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SMILES
N#CC1(C(N2C[C@]3([H])CCOC4=CC5=NC(C)=NC(N[C@@H](C6=CC=CC(C(F)F)=C6F)C)=C5C=C4N3CC2)=O)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 250 mg/mL (454.07 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, 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 (279 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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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 | 1.8163 mL | 9.0815 mL | 18.1630 mL | 45.4075 mL |
| 5 mM | 0.3633 mL | 1.8163 mL | 3.6326 mL | 9.0815 mL | |
| 10 mM | 0.1816 mL | 0.9081 mL | 1.8163 mL | 4.5407 mL | |
| 15 mM | 0.1211 mL | 0.6054 mL | 1.2109 mL | 3.0272 mL | |
| 20 mM | 0.0908 mL | 0.4541 mL | 0.9081 mL | 2.2704 mL | |
| 25 mM | 0.0727 mL | 0.3633 mL | 0.7265 mL | 1.8163 mL | |
| 30 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5136 mL | |
| 40 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1352 mL | |
| 50 mM | 0.0363 mL | 0.1816 mL | 0.3633 mL | 0.9081 mL | |
| 60 mM | 0.0303 mL | 0.1514 mL | 0.3027 mL | 0.7568 mL | |
| 80 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL | |
| 100 mM | 0.0182 mL | 0.0908 mL | 0.1816 mL | 0.4541 mL |
SOS1-IN-14 Related Classifications
HY-151517 Related Classifications
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