BRK inhibitor P21d hydrochloride

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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.

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BRK inhibitor P21d hydrochloride Chemical Structure

CAS No. : 2250025-98-8

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Description	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].
IC₅₀ & Target	IC50: 30 nM (BRK), 52 nM (p-SAM68), >20 μM (Aurora B), >20 μM (Lck)^[1]
In Vitro	BRK inhibitor P21d hydrochloride (compound 21d) inhibits Aurora B (IC₅₀>20 μM) and Lck (IC₅₀>20 μM)^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. BRK inhibitor P21d hydrochloride Related Antibodies
In Vivo	BRK inhibitor P21d hydrochloride (compound 21d) has much better permeability (CACO-2:314 nm/s) and PK profile (rat, po, 10 mpk, AUC_0–6h=31.1 μM•h,C_6h=3.5 μM)^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	483.93
Formula	C₂₃H₂₃ClFN₇O₂
CAS No.	2250025-98-8
Appearance	Solid
Color	White to off-white
SMILES	O=C(C1=CC=C(NC2=NC(C3CC3)=CN4C2=NC=C4C5=CNN=C5)C(F)=C1)N6CCOCC6.[H]Cl
Shipping	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)
Purity & Documentation	Purity: ≥98.0% Select Batch: Data Sheet (273 KB) SDS (251 KB) COA (255 KB) Elemental Analysis Report (113 KB) Handling Instructions (2659 KB)
References	[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. [Content Brief]