RK-24466 (KIN 001-51, Lck inhibitor C8863, C8863) is a potent and selective Lck inhibitor that inhibits two human Lck kinase builders, lck (64-509) and lckcd. The corresponding IC50 values are less than 0.001 μM and 0.002 μM, respectively.

 

Brand: BCM

 

Target: Src

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: RK-24466, a lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, significantly inhibited both VSMC proliferation and migration. RK-24466 suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreased the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb). Additionally, RK-24466 suppressed the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury. The present study identified RK-24466 as a potent VSMC proliferation and migration inhibitor and warrants further studies to elucidate its more detailed molecular mechanisms, such as its primary target, and to further validate its in vivo efficacy as a therapeutic agent for pathologic vascular conditions, such as restenosis and atherosclerosis.

 

Boiling Point: 605.1±55.0 °C(Predicted)

 

pKa: 5.75±0.30(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: C1CCC(C1)N2C=C(C3=C(N=CN=C32)N)C4=CC=C(C=C4)OC5=CC=CC=C5  

 

InChIKey: FMETVQKSDIOGPX-UHFFFAOYSA-N  

 

InChI: InChI=1S/C23H22N4O/c24-22-21-20(14-27(17-6-4-5-7-17)23(21)26-15-25-22)16-10-12-19(13-11-16)28-18-8-2-1-3-9-18/h1-3,8-15,17H,4-7H2,(H2,24,25,26) 

 

Attribute
[Chem Name]	7-cyclopentyl-5-(4-phenoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
[Synonym]	RK 24466; KIN 001-51; Lck inhibitor C 8863; C8863
[CAS No.]	213743-31-8
[MDL No.]	MFCD04974490
[Formula]	C23H22N4O
[Molecular]	370.45
[Form]	White solid
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C

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