UNC9426
Based on 1 Customer Validation
UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.51%
- CAS. Nr.: 3051784-94-9
- Formel: C32H34F6N6O
- Molecular Weight:632.64
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Help & FAQs
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Kinase Inhibitor Library
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Biologische Aktivität
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Tyro3 2.1 nM (IC50) |
Axl 190 nM (IC50) |
MERTK 580 nM (IC50) |
UNC9426 (compound 12) (0.5 nM-10 μM) exhibits differential binding potency against the three TAM kinase family members (TYRO3, MERTK, and AXL), as evidenced by its highest affinity for TYRO3 (EC50 = 89.8 nM)[1].
UNC9426 (10 μM, 10 min) inhibits human platelet aggregation and reduces the expression of human platelet surface activation markers PAC-1 and P-selectin[1].
UNC9426 (100-10000 nM, 0-10 h) significantly inhibits the efferocytosis activity in macrophages in THP1 cells[1].
UNC9426 (30-10000 nM, 7-10 days) exhibits potent inhibition of colony formation in NSCLC cell cultures with EC50 values of 170 nM (H1650) and 197 nM (H1975)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | AUClast | Vss | CL | F |
|---|---|---|---|---|---|---|---|---|
| Mice | 3 mg/kg | i.v. | 10.0 h | 3.4 μM | 18.7 μM·h | 2.6 L/kg | 3.5 mL/min/kg | / |
| Mice | 3 mg/kg | p.o. | 9.4 h | 0.35 μM | 6.76 μM·h | / | / | 36 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wildtype C57BL/6 mice (6-12 weeks)[1]
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Dosage:10 mg/kg
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Administration:i.v.
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Result:Reduced the total bleeding duration and the time until initial cessation of bleeding in mice compared to the control.
Showed no significantly affect on the number of rebleeding events in mice during the 15-minute experimental period.
Chemical Information
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CAS. Nr. 3051784-94-9
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Appearance Solid
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Molecular Weight 632.64
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Formel C32H34F6N6O
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Color White to off-white
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SMILES
O[C@H](CC1)CC[C@@H]1N2C=C(C3=CC=C(C=C3)CN4CCN(CC4)C)C5=CN=C(N=C52)NC6=CC(C(F)(F)F)=CC(C(F)(F)F)=C6
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 20.59 mg/mL (32.55 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (276 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)
Verweise
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 | 1.5807 mL | 7.9034 mL | 15.8068 mL | 39.5169 mL |
| 5 mM | 0.3161 mL | 1.5807 mL | 3.1614 mL | 7.9034 mL | |
| 10 mM | 0.1581 mL | 0.7903 mL | 1.5807 mL | 3.9517 mL | |
| 15 mM | 0.1054 mL | 0.5269 mL | 1.0538 mL | 2.6345 mL | |
| 20 mM | 0.0790 mL | 0.3952 mL | 0.7903 mL | 1.9758 mL | |
| 25 mM | 0.0632 mL | 0.3161 mL | 0.6323 mL | 1.5807 mL | |
| 30 mM | 0.0527 mL | 0.2634 mL | 0.5269 mL | 1.3172 mL |
UNC9426 Related Classifications
HY-173268 Related Classifications
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