TYRA-200
Based on 1 Customer Validation
TYRA-200 is a potent and orally active FGFR2 inhibitor. TYRA-200 inhibits the kinase activity of wild-type FGFR2 and its mutants. TYRA-200 induces significant tumor regression in FGFR2-driven cancer models. TYRA-200 can be used for the research of FGFR2-altered advanced solid tumors, intrahepatic cholangiocarcinoma, and endometrial cancer.
For research use only. We do not sell to patients.
- Purity: 98.06%
- CAS No.: 2823289-77-4
- Formula: C23H24FN7O2
- Molecular Weight:449.48
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Storage: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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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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Kinase Inhibitor Library
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Anti-Cancer Compound Library
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Clinical Compound Library
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Orally Active Compound Library
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Angiogenesis-Related Compound Library
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Anti-Liver Cancer Compound Library
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Anti-Prostate Cancer Compound Library
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Anti-Pulmonary Fibrosis Compound Library
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
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Highly Selective Inhibitors Library
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High-Throughput Bioactive Compound Library
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Biological Activity
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FGFR2 |
TYRA-200 potently inhibits the enzymatic activity of FGFR2 gatekeeper mutants (V565L, V565F) and molecular brake mutants (N550D, N550H, N550K, E566A), and exhibits potent cellular growth inhibitory activity against Ba/F3 cells expressing FGFR2 variants N550K, V565F, V565I, K660E, and K660N[2].
TYRA-200 maintains in vitro activity in AN3CA endometrial cancer cells harboring the FGFR2 N550K molecular brake mutation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2823289-77-4
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Appearance Powder
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Molecular Weight 449.48
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Formula C23H24FN7O2
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Color Off-white to light yellow
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SMILES
C=CC(NC1=CC2=C(N(C=C2C)C3=C(C=NC(NC4=CN(N=C4)CC(C)(O)C)=N3)F)C=C1)=O
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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 : 100 mg/mL (222.48 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.12 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 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)
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 | 2.2248 mL | 11.1240 mL | 22.2479 mL | 55.6198 mL |
| 5 mM | 0.4450 mL | 2.2248 mL | 4.4496 mL | 11.1240 mL | |
| 10 mM | 0.2225 mL | 1.1124 mL | 2.2248 mL | 5.5620 mL | |
| 15 mM | 0.1483 mL | 0.7416 mL | 1.4832 mL | 3.7080 mL | |
| 20 mM | 0.1112 mL | 0.5562 mL | 1.1124 mL | 2.7810 mL | |
| 25 mM | 0.0890 mL | 0.4450 mL | 0.8899 mL | 2.2248 mL | |
| 30 mM | 0.0742 mL | 0.3708 mL | 0.7416 mL | 1.8540 mL | |
| 40 mM | 0.0556 mL | 0.2781 mL | 0.5562 mL | 1.3905 mL | |
| 50 mM | 0.0445 mL | 0.2225 mL | 0.4450 mL | 1.1124 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3708 mL | 0.9270 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2781 mL | 0.6952 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2225 mL | 0.5562 mL |
TYRA-200 Related Classifications
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