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.
For research use only. We do not sell to patients.
- CAS No.: 1454584-91-8
- Formula: C23H21ClFN9
- Molecular Weight:477.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CK1δ 4 nM (IC50) |
CK1ε 44 nM (IC50) |
Cdk4/cyclin D1 283 nM (IC50) |
Cdk4/cyclin D3 368 nM (IC50) |
CK1ε 14 nM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | CL | AUC | T1/2 | F |
|---|---|---|---|---|---|---|---|
| Mice[1] | 1 nM | i.v. | 4.6 μM | 8.4 mL/min/kg | 4.16 μM·h | 1.50 h | 10 % |
Chemical Information
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CAS No. 1454584-91-8
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Molecular Weight 477.92
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Formula C23H21ClFN9
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SMILES
FC1=CC(N2C=NC3=C(NCC4=NC5=CC(Cl)=CC=C5N4)N=C(N6CCNCC6)N=C23)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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