TAK-285
Based on 3 publication(s) in Google Scholar
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.99%
- No. CAS: 871026-44-7
- Fòrmula: C26H25ClF3N5O3
- Peso molecular:547.96
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) TAK-285
MoreVer todos los productos específicos de isoformas EGFR
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Actividad biológica
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EGFR 23 nM (IC50) |
HER2 17 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | GI50 |
17 nM
Compound: 34e, TAK-285
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Growth inhibition of human BT474 cells overexpressing HER2 gene after 5 days by particle analyzer
Growth inhibition of human BT474 cells overexpressing HER2 gene after 5 days by particle analyzer
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[PMID: 22003817] |
| BT-474 | GI50 |
17 nM
Compound: TAK-285
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Growth inhibition of human BT474 cells overexpressing HER2 after 5 days
Growth inhibition of human BT474 cells overexpressing HER2 after 5 days
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[PMID: 23490150] |
| Sf9 | IC50 |
4 nM
Compound: 1, TAK-285
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Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
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[PMID: 24900643] |
| Sf9 | IC50 |
8400 nM
Compound: 1, TAK-285
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Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
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[PMID: 24900643] |
TAK-285 (Compound 34e) shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM[1]. TAK-285 (Compound 34e) exhibits HER4 inhibitory activity with an IC50 value of 260 nM. TAK-285 also inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK and Lyn B with IC50s of 1100 nM, 5700 nM, 4200 nM, 1700 nM, 2400 nM, 4700 nM and 5200 nM, respectively[1].
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.
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Animal Model:Female BALB/cAJcl mice (7-weeks old) with 4−1ST xenograft models[1]
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Dosage:50 mg/kg, 100 mg/kg
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Administration:Oral administration; twice daily; for 14 days
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Result:Exhibited dose-dependent tumor growth inhibition.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 871026-44-7
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Appearance Solid
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Peso molecular 547.96
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Fòrmula C26H25ClF3N5O3
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Color White to light yellow
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SMILES
ClC(C=C(NC1=NC=NC2=C1N(CCNC(CC(C)(C)O)=O)C=C2)C=C3)=C3OC4=CC=CC(C(F)(F)F)=C4
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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 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jan;649(8098):1032-1041. PMID: 41299171 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
iScience
FUS-dependent microRNA deregulations identify TRIB2 as a druggable target for ALS motor neurons. [Abstract]2023 Oct 6;26(11):108152. PMID: 37920668
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (91.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ishikawa T, et al. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J Med Chem. 2011 Dec 8;54(23):8030-50. [Content Brief]
[2]. Erdo F, et al. Verification of brain penetration of the unbound fraction of a novel HER2/EGFR dual kinase inhibitor (TAK-285) by microdialysis in rats. Brain Res Bull. 2012 Mar 10;87(4-5):413-9. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8250 mL | 9.1248 mL | 18.2495 mL | 45.6238 mL |
| 5 mM | 0.3650 mL | 1.8250 mL | 3.6499 mL | 9.1248 mL | |
| 10 mM | 0.1825 mL | 0.9125 mL | 1.8250 mL | 4.5624 mL | |
| 15 mM | 0.1217 mL | 0.6083 mL | 1.2166 mL | 3.0416 mL | |
| 20 mM | 0.0912 mL | 0.4562 mL | 0.9125 mL | 2.2812 mL | |
| 25 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8250 mL | |
| 30 mM | 0.0608 mL | 0.3042 mL | 0.6083 mL | 1.5208 mL | |
| 40 mM | 0.0456 mL | 0.2281 mL | 0.4562 mL | 1.1406 mL | |
| 50 mM | 0.0365 mL | 0.1825 mL | 0.3650 mL | 0.9125 mL | |
| 60 mM | 0.0304 mL | 0.1521 mL | 0.3042 mL | 0.7604 mL | |
| 80 mM | 0.0228 mL | 0.1141 mL | 0.2281 mL | 0.5703 mL |
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