Labuxtinib
Based on 1 Customer Validation
Labuxtinib (EVT-8565072; THB335) is a potent dual inhibitor of c-Kit and PDGFR. Labuxtinib exhibits potent inhibitory activity against wild-type c-Kit (IC50 = 0.005 μM). Labuxtinib inhibits SCF-dependent and PDGF-dependent cell proliferation, and blocks the proliferation of cells dependent on c-Kit or PDGFR signaling pathways. In animal models of skin allergy, Labuxtinib depletes skin mast cells and significantly alleviates anaphylactic shock responses. Labuxtinib can be used in research on mast cell-related diseases, respiratory diseases, inflammatory diseases, fibrotic diseases, metabolic diseases, and other related conditions.
For research use only. We do not sell to patients.
- Purity: 98.74%
- CAS No.: 1426449-01-5
- Formula: C20H16FN5O2
- Molecular Weight:377.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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PDGFR |
Labuxtinib (F13) inhibits SCF-dependent proliferation in human Mo7e cells and PDGF-dependent proliferation in rat A10 cells and human TG/HA-VSMC cells[1].
Labuxtinib blocks the proliferation of cells dependent on c-Kit or PDGFR signaling pathways and shows potent c-Kit inhibitory activity with an IC50 value of 7 nM[1].
Labuxtinib (THB33) acts as a competitive inhibitor at the KIT ATP-binding pocket to block KIT signaling[3][4].
Labuxtinib inhibits wild-type KIT phosphorylation and KIT-dependent cellular activity, with IC50 values of 0.005 μM and 0.0079 μM respectively[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Labuxtinib induces dose-dependent depletion of dermal mast cells and reduces cutaneous anaphylaxis in a rat passive cutaneous anaphylaxis model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1426449-01-5
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Appearance Solid
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Molecular Weight 377.37
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Formula C20H16FN5O2
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Color White to light yellow
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SMILES
CC1=CC=C(C2=NOC([C@@H]3[C@H](C3)F)=N2)C=C1NC(C4=CN=C5N4C=CC=C5)=O
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Synonyms
EVT-8565072; THB335
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (331.24 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)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 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. 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 | 2.6499 mL | 13.2496 mL | 26.4992 mL | 66.2480 mL |
| 5 mM | 0.5300 mL | 2.6499 mL | 5.2998 mL | 13.2496 mL | |
| 10 mM | 0.2650 mL | 1.3250 mL | 2.6499 mL | 6.6248 mL | |
| 15 mM | 0.1767 mL | 0.8833 mL | 1.7666 mL | 4.4165 mL | |
| 20 mM | 0.1325 mL | 0.6625 mL | 1.3250 mL | 3.3124 mL | |
| 25 mM | 0.1060 mL | 0.5300 mL | 1.0600 mL | 2.6499 mL | |
| 30 mM | 0.0883 mL | 0.4417 mL | 0.8833 mL | 2.2083 mL | |
| 40 mM | 0.0662 mL | 0.3312 mL | 0.6625 mL | 1.6562 mL | |
| 50 mM | 0.0530 mL | 0.2650 mL | 0.5300 mL | 1.3250 mL | |
| 60 mM | 0.0442 mL | 0.2208 mL | 0.4417 mL | 1.1041 mL | |
| 80 mM | 0.0331 mL | 0.1656 mL | 0.3312 mL | 0.8281 mL | |
| 100 mM | 0.0265 mL | 0.1325 mL | 0.2650 mL | 0.6625 mL |
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