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BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK/PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $964 | 3-6 months | 3-6 months |
| Description | BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK/PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment. |
| Targets&IC50 | Aurora B:>20 μM (IC50), pSAM68:52 nM (IC50), Brk:30 nM (IC50), Lck:>20 μM (IC50) |
| In vitro | BRK inhibitor P21d hydrochloride (compound 21d) inhibits Aurora B and Lck with an IC50 of greater than 20 μM for each target[1]. |
| In vivo | The BRK inhibitor P21d hydrochloride, also known as compound 21d, demonstrates significantly enhanced permeability (CACO-2: 314 nm/s) and pharmacokinetic (PK) properties. When administered orally at a dose of 10 mpk in rats, it exhibits an AUC from 0 to 6 hours of 31.1 μM·h and a concentration of 3.5 μM at the 6-hour mark [1]. |
| Synonyms | BRK inhibitor P21d hydrochloride |
| Molecular Weight | 483.93 |
| Formula | C23H23ClFN7O2 |
| Cas No. | 2250025-98-8 |
| Smiles | Cl.Fc1cc(ccc1Nc1nc(cn2c(cnc12)-c1cn[nH]c1)C1CC1)C(=O)N1CCOCC1 |
| 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. |
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.
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.
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