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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 | Availability | Quantity |
---|---|---|---|
25 mg | $964 | 8-10 weeks |
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), Brk:30 nM (IC50), pSAM68:52 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]. |
Alias | BRK inhibitor P21d hydrochloride |
Molecular Weight | 483.93 |
Formula | C23H23ClFN7O2 |
Cas No. | 2250025-98-8 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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