SR-2890
CAS No. : 1454584-91-8
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| Cat. No. : | HY-123859 |
| M.Wt: | 477.92 |
| Formula: | C23H21ClFN9 |
| Purity: | >98 % |
| Solubility: |
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].
In Vitro:SR-2890 inhibits proliferation of human A375 melanoma cells (EC50 = 38 nM)[1].
SR-2890 exhibits human liver microsome stability, solubility, without CYP inhibition (T1/2 = 44 min; solubility = 60 μM; CYP inhibition >10 μM)[1].
SR-2890 weakly inhibits off-target kinases FLT3 (IC50=809 nM), CDK4/cyclin D1 (IC50=283 nM) and CDK4/cyclin D3 (IC50=368 nM)[1].
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