Tuxobertinib
Based on 1 publication(s) in Google Scholar
Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
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- Pureza: 99.88%
- No. CAS: 2414572-47-5
- Fòrmula: C29H29ClN6O4
- Peso molecular:561.03
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Tuxobertinib
MoreVer todos los productos específicos de isoformas EGFR
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Actividad biológica
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EGFR 0.2 nM (Kd) |
HER2 0.76 nM (Kd) |
RIPK2 1.2 nM (Kd) |
BLK 13 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
~ 1 μM
Compound: BDTX-189
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Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR
Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR
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[PMID: 37669428] |
Tuxobertinib is a masterKey inhibitor of the ERBB allosteric mutant oncogene family with antiproliferative activity (IC50<100 nM for ERBB allosteric mutant oncogene family)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? Tuxobertinib (1-50 mg/kg.p.o.; daily for 15 days) shows dose-dependent tumor growth inhibition and regression in athymic nude mice bearing CUTO-14 PDX tumors that express the EGFR mutation EGFR ASV[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2414572-47-5
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Appearance Solid
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Peso molecular 561.03
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Fòrmula C29H29ClN6O4
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Color Off-white to light yellow
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SMILES
C=CC(NC1=CC2=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)N=CN=C2C=C1OCCN5CCOCC5)=O
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Synonyms
BDTX-189
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 41.67 mg/mL (74.27 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: 2.08 mg/mL (3.71 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (274 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)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7824 mL | 8.9122 mL | 17.8244 mL | 44.5609 mL |
| 5 mM | 0.3565 mL | 1.7824 mL | 3.5649 mL | 8.9122 mL | |
| 10 mM | 0.1782 mL | 0.8912 mL | 1.7824 mL | 4.4561 mL | |
| 15 mM | 0.1188 mL | 0.5941 mL | 1.1883 mL | 2.9707 mL | |
| 20 mM | 0.0891 mL | 0.4456 mL | 0.8912 mL | 2.2280 mL | |
| 25 mM | 0.0713 mL | 0.3565 mL | 0.7130 mL | 1.7824 mL | |
| 30 mM | 0.0594 mL | 0.2971 mL | 0.5941 mL | 1.4854 mL | |
| 40 mM | 0.0446 mL | 0.2228 mL | 0.4456 mL | 1.1140 mL | |
| 50 mM | 0.0356 mL | 0.1782 mL | 0.3565 mL | 0.8912 mL | |
| 60 mM | 0.0297 mL | 0.1485 mL | 0.2971 mL | 0.7427 mL |
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