Lck inhibitor 2

Modify Date: 2024-01-09 10:42:19

Lck inhibitor 2 structure	Common Name	Lck inhibitor 2
	CAS Number	944795-06-6	Molecular Weight	335.36000
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₈H₁₇N₅O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Lck inhibitor 2

Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively IC50 Value: 13 nM(Lck) [1]Target: Src family kinaseLck inhibitor 2(Compound 9) inhibited 48 kinases with %control < 1 (33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). A further 27 kinases were bound with %control < 10. Kd values for 16 kinases were determined and found to be below 100 nM. These included TXK (10 nM)[2].

Name	3-({4-[(5-Hydroxy-2-methylphenyl)amino]-2-pyrimidinyl}amino)benza mide
Synonym	More Synonyms

Description	Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively IC50 Value: 13 nM(Lck) [1]Target: Src family kinaseLck inhibitor 2(Compound 9) inhibited 48 kinases with %control < 1 (33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). A further 27 kinases were bound with %control < 10. Kd values for 16 kinases were determined and found to be below 100 nM. These included TXK (10 nM)[2].
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src Research Areas >> Inflammation/Immunology
References	[1]. Bamborough, et al. Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery. Journal of Medicinal Chemistry (2008), 51(24), 7898-7914. [2]. Bamborough, Paul, et al. N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics. Bioorganic & Medicinal Chemistry Letters (2007), 17(15), 4363-4368. [3]. Awale, Mahendra, et al. Molecular docking guided 3D-QSAR CoMFA analysis of N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of leukocyte-specific protein tyrosine kinase. Journal of Molecular Modeling (2008), 14(10), 937-947.

Description

Related Catalog

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

Research Areas >> Inflammation/Immunology

References

[1]. Bamborough, et al. Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery. Journal of Medicinal Chemistry (2008), 51(24), 7898-7914.

[2]. Bamborough, Paul, et al. N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics. Bioorganic & Medicinal Chemistry Letters (2007), 17(15), 4363-4368.

[3]. Awale, Mahendra, et al. Molecular docking guided 3D-QSAR CoMFA analysis of N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of leukocyte-specific protein tyrosine kinase. Journal of Molecular Modeling (2008), 14(10), 937-947.