QL47

Names

[ Name ]:
QL47

[Synonym ]:
1-(1-Acryloyl-2,3-dihydro-1H-indol-6-yl)-9-(1-methyl-1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-2(1H)-one
Benzo[h]-1,6-naphthyridin-2(1H)-one, 1-[2,3-dihydro-1-(1-oxo-2-propen-1-yl)-1H-indol-6-yl]-9-(1-methyl-1H-pyrazol-4-yl)-
9-(1-methyl-4-pyrazolyl)-1-[1-(1-oxoprop-2-enyl)-2,3-dihydroindol-6-yl]-2-benzo[h][1,6]naphthyridinone

Biological Activity

[Description]:

QL47 is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM.IC50 Value: 7 nMTarget: Btkin vitro: QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces a G1 cell cycle arrest which is associated with pronounced degradation of BTK protein. QL47 inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations [1].in vivo: N/A

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

Research Areas >> Cancer

[References]

[1]. Wu, H., et al., Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma. ACS Chem Biol, 2014.

[Related Small Molecules]

Acalabrutinib | GDC-0853 | Evobrutinib | AVL-292 | (±)-Zanubrutinib | ONO-4059 | BMX-IN-1 | GDC-0834 | SNS-062 | RN486 | LFM-A13 | Vecabrutinib | CGI-1746 | BMS-986195 | CNX-774

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
706.2±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₇H₂₁N₅O₂

[ Molecular Weight ]:
447.488

[ Flash Point ]:
380.9±32.9 °C

[ Exact Mass ]:
447.169525

[ LogP ]:
2.50

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.724

[ Storage condition ]:
2-8℃