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BRK inhibitor P21d hydrochloride

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Catalog No. T39772Cas No. 2250025-98-8
Alias BRK inhibitor P21d hydrochloride

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.

BRK inhibitor P21d hydrochloride

BRK inhibitor P21d hydrochloride

😃Good
Catalog No. T39772Alias BRK inhibitor P21d hydrochlorideCas No. 2250025-98-8
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.
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25 mg$9648-10 weeks
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Product Introduction

Bioactivity
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].
AliasBRK inhibitor P21d hydrochloride
Chemical Properties
Molecular Weight483.93
FormulaC23H23ClFN7O2
Cas No.2250025-98-8
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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