1454584-91-8
Chemical Structure
SR-2890
- CAS No.: 1454584-91-8
- Formula:C23H21ClFN9
- Molecular Weight:477.92
IUPAC Name: N-((5-chloro-1H-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-(piperazin-1-yl)-9H-purin-6-amine
InChIKey: NGIQKILKGCPSJO-UHFFFAOYSA-N
SMILES: FC1=CC(N2C=NC3=C(NCC4=NC5=CC(Cl)=CC=C5N4)N=C(N6CCNCC6)N=C23)=CC=C1
Biological Activity: SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease[1].
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SR-2890 | SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease. | |||||||||||||||||||||
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