SR-1277

Names

[ Name ]:
SR-1277

Biological Activity

[Description]:

SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase

Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase

[Target]

CKIδ:49 nM (IC50)

CKIϵ:260 nM (IC50)

[In Vitro]

SR-1277 exhibits antiproliferative effects in A375 cells, with an EC50 of 22 nM[1].

[In Vivo]

SR-1277 (1 mg/kg; i.v.) exhibits Cmax (1.2 μM), Cl (2.8 ml/min/kg), AUC(1.26 μM•h), T1/2 (1.42 h) and brain penetration (24%) in mice[1].

[References]

[1]. Bibian M, et, al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₁₉N₉O₃S

[ Molecular Weight ]:
477.50

Related Compounds

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