SR-1277

Modify Date: 2024-04-05 18:17:57

SR-1277 Structure
SR-1277 structure
Common Name SR-1277
CAS Number 1446715-47-4 Molecular Weight 477.50
Density N/A Boiling Point N/A
Molecular Formula C21H19N9O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SR-1277


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].

 Names

Name SR-1277

 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
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