| Bioactivity | BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models[1]. |
| Target | IC50: 30 nM (BRK), 52 nM (p-SAM68), >20 μM (Aurora B), >20 μM (Lck) |
| Invitro | BRK inhibitor P21d hydrochloride (compound 21d) inhibits Aurora B (IC50>20 μM) and Lck (IC50>20 μM)[1]. |
| In Vivo | BRK inhibitor P21d hydrochloride (compound 21d) has much better permeability (CACO-2:314 nm/s) and PK profile (rat, po, 10 mpk, AUC0–6h=31.1 μM•h,C6h=3.5 μM)[1]. |
| Name | BRK inhibitor P21d hydrochloride |
| CAS | 2250025-98-8 |
| Formula | C23H23ClFN7O2 |
| Molar Mass | 483.93 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Hongbo Zeng, et al. Discovery of Novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 Inhibitors. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5. |