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Takeda103A
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Catalog No. T24850Cas No. 865609-72-9
Alias Takeda-103-A, Takeda-103A, Takeda 103 A, CMPD-103A, CMPD103A
Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.
Takeda103A
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Purity: 97.17%
Catalog No. T24850Alias Takeda-103-A, Takeda-103A, Takeda 103 A, CMPD-103A, CMPD103ACas No. 865609-72-9
Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $77 | In Stock | In Stock | |
| 2 mg | $107 | In Stock | In Stock | |
| 5 mg | $167 | In Stock | In Stock | |
| 10 mg | $271 | In Stock | In Stock | |
| 25 mg | $446 | In Stock | In Stock | |
| 50 mg | $592 | In Stock | In Stock | |
| 100 mg | $828 | - | In Stock | |
| 200 mg | $1,090 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $196 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:97.17%
Appearance:Solid
Color:White
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Product Introduction
Takeda103A AI Summary
Takeda103A exhibits potent inhibitory activity against various kinases. It strongly inhibits full-length human G protein-coupled receptor kinase 2 (GRK2), including the S670A mutant, with an IC50 of 20.0 nM and a dissociation constant (Kd) of 1.99 nM as determined by Thermofluor thermal shift assay. The compound also inhibits recombinant human N-terminal GST-tagged GRK2 with an IC50 of 1.2 nM as measured by the Lance TR-FRET assay. It demonstrates moderate inhibitory activity against GRK5 (IC50 of 2200.0 nM), ROCK2 (IC50 of 190.0 nM), and PKCalpha (IC50 of 250.0 nM), while showing less inhibition on GRK1 (IC50 of 9000.0 nM). Additionally, Takeda103A inhibits CYP3A4 with an inhibition rate of 51.0% at a concentration of 10 uM. In terms of ROCK1, it shows only 10.0% inhibition at 10 uM via ADP-Glo kinase assay. The selectivity ratio of IC50 for PKA to IC50 for full-length GRK2 (S670A mutant) is 50.0..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor. |
| Synonyms | Takeda-103-A, Takeda-103A, Takeda 103 A, CMPD-103A, CMPD103A |
| Molecular Weight | 463.48 |
| Formula | C24H23F2N7O |
| Cas No. | 865609-72-9 |
| Smiles | CCCn1c(CNc2cccc(c2)C(=O)NCc2c(F)cccc2F)nnc1-c1ccncn1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 11 mg/mL (23.73 mM), Sonication is recommended.  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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