BRK inhibitor P21d hydrochloride

Modify Date: 2025-08-26 19:03:55

BRK inhibitor P21d hydrochloride Structure
BRK inhibitor P21d hydrochloride structure
Common Name BRK inhibitor P21d hydrochloride
CAS Number 2250025-98-8 Molecular Weight 483.93
Density N/A Boiling Point N/A
Molecular Formula C23H23ClFN7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BRK inhibitor P21d hydrochloride


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].

 Names

Name BRK inhibitor P21d hydrochloride

 BRK inhibitor P21d hydrochloride Biological Activity

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].
Related Catalog
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].
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].
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.

 Chemical & Physical Properties

Molecular Formula C23H23ClFN7O2
Molecular Weight 483.93
InChIKey GWHGHKMCIUENCZ-UHFFFAOYSA-N
SMILES Cl.O=C(c1ccc(Nc2nc(C3CC3)cn3c(-c4cn[nH]c4)cnc23)c(F)c1)N1CCOCC1
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