PeptideDB

BRK inhibitor P21d hydrochloride

CAS: 2250025-98-8 F: C23H23ClFN7O2 W: 483.93

BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibit
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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.