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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.74%
- CAS 番号: 1426449-01-5
- 分子式: C20H16FN5O2
- 分子量:377.37
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[2]|
PDGFR |
体外実験
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.
体内実験
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.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
化学情報
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CAS 番号 1426449-01-5
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性状 Solid
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分子量 377.37
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分子式 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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別名
EVT-8565072; THB335
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
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| 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 |
Labuxtinib 関連分類
HY-156619 関連分類
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