Fudotinib
Based on 1 Customer Validation
Fudotinib (JYP0322) (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. Fudotinib selectively inhibits human wild-type ROS1 and human ROS1G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. Fudotinib inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. Fudotinib can be used for the research of non-small cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- Purity : 98.59%
- CAS No.: 2644645-39-4
- Formula: C20H16FN7O3
- Molecular Weight:421.38
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TrkA |
TrkB |
TrkC |
In Vitro
Fudotinib (JYP0322) inhibits wild-type ROS1 and ROS1G2032R with high selectivity, showing 130-fold, 20-fold, and 6-fold selectivity over TRKA, TRKB, and TRKC, respectively[1].
Fudotinib (0-1 μM; 3 days) potently inhibited CD74-ROS1-driven Ba/F3 cells (wild-type and mutants), while showing reduced activity against TRK-driven Ba/F3 LMNA-NTRK1 cells, maintaining ROS1 selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 LMNA-NTRK1; wild-type Ba/F3 cells
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Concentration:0-1 μM
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Incubation Time:3 days
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Result:Showed reduced potency against Ba/F3 LMNA-NTRK1 cells (IC50 = 37 nM) compared to Repotrectinib (HY-103022) (IC50 = 1.1 nM).
Inhibited proliferation of Ba/F3 cells expressing wild-type CD74-ROS1 and clinically relevant ROS1 mutations.
In Vivo
Fudotinib (1, 3, and10 mg/kg; p.o.; twice daily for 5 weeks) induces dose-dependent tumor growth inhibition in mouse LU-01-0414 SDC4-ROS1 PDX xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c Nude mice (6-8 weeks old) subcutaneously injected with CD74-ROS1WT cells[1]
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Dosage:1.5; 5; 15 mg/kg
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Administration:p.o.; BID for 2 weeks
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Result:Achieved tumor growth inhibition (TGI) rates of 83.5%, 101.4%, and 103.4% at doses of 1.5, 5, and 15 mg/kg BID, respectively.
Demonstrated efficacy at 5 mg/kg comparable to Crizotinib (HY-50878).
Caused no significant weight loss or observable adverse effects.
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Animal Model:Female BALB/c Nude mice (6-8 weeks old) subcutaneously implanted with LU-01-0414 SDC4-ROS1 tumor fragments[1]
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Dosage:1; 3; 10 mg/kg
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Administration:p.o.; BID for 5 weeks
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Result:Achieved TGI rates of 87.3% at 3 mg/kg, comparable to Entrectinib (HY-12678).
Achieved TGI rates of 94.2% at 10 mg/kg, comparable to Repotrectinib.
Caused no significant weight loss or observable adverse effects.
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Animal Model:Female NOD SCID mice (6-8 weeks old) subcutaneously injected with Ba/F3 CD74-ROS1G2032R cells[1]
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Dosage:1.5; 5; 15 mg/kg
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Administration:p.o.; BID for 2 weeks
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Result:Induced tumor regression at doses of 5 and 15 mg/kg, achieving TGI rates of 81.7% and 100.3%, respectively.
Demonstrated superior efficacy to Taletrectinib (HY-131003) and Repotrectinib.
Caused no significant weight loss or observable adverse effects.
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2644645-39-4
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Appearance Solid
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Molecular Weight 421.38
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Formula C20H16FN7O3
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Color White to off-white
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SMILES
N#CC1=NN2C=CC3=NC2=C1C(NC4(COC5=NC=C(C=C5[C@H]6CCON36)F)CC4)=O
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Synonyms
JYP0322
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 16.67 mg/mL (39.56 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)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.3732 mL | 11.8658 mL | 23.7315 mL | 59.3289 mL |
| 5 mM | 0.4746 mL | 2.3732 mL | 4.7463 mL | 11.8658 mL | |
| 10 mM | 0.2373 mL | 1.1866 mL | 2.3732 mL | 5.9329 mL | |
| 15 mM | 0.1582 mL | 0.7911 mL | 1.5821 mL | 3.9553 mL | |
| 20 mM | 0.1187 mL | 0.5933 mL | 1.1866 mL | 2.9664 mL | |
| 25 mM | 0.0949 mL | 0.4746 mL | 0.9493 mL | 2.3732 mL | |
| 30 mM | 0.0791 mL | 0.3955 mL | 0.7911 mL | 1.9776 mL |
Fudotinib Related Classifications
HY-176942 Related Classifications
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