| Identification | Back Directory | [Name]
Methanone, [4-[[6-cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-fluorophenyl]-4-morpholinyl-, hydrochloride (1:1) | [CAS]
2250025-98-8 | [Synonyms]
BRK inhibitor P21d hydrochloride
Methanone, [4-[[6-cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-fluorophenyl]-4-morpholinyl-, hydrochloride (1:1) | [Molecular Formula]
C23H23ClFN7O2 | [MOL File]
2250025-98-8.mol | [Molecular Weight]
483.93 |
| Hazard Information | Back Directory | [Description]
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor. It can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models. | [Uses]
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]. | [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. DOI:10.1016/j.bmcl.2011.07.101 |
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