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SR-1277 is a potent, highly selective and ATP-competitive CK1δ/ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.CK1δ plays a crucial role in regulating Wee1 activity at the G2/M cell-cycle interface, and exhibits significant antiproliferative activity against a variety of cancer cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $397 | In Stock | |
5 mg | $970 | In Stock | |
10 mg | $1,290 | In Stock | |
25 mg | $1,950 | In Stock | |
50 mg | $2,620 | In Stock | |
100 mg | $3,530 | In Stock |
Description | SR-1277 is a potent, highly selective and ATP-competitive CK1δ/ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.CK1δ plays a crucial role in regulating Wee1 activity at the G2/M cell-cycle interface, and exhibits significant antiproliferative activity against a variety of cancer cells. |
Targets&IC50 | CKIδ:49 nM, CKIϵ:260 nM |
In vitro | Methods: A375 cells were treated with SR-1277 and cell viability was determined by MTT assay. Results: SR-1277 showed antiproliferative effects in A375 cells with an EC50 value of 22 nM. [1] |
In vivo | Methods: SR-1277 (1 mg/kg, intravenous injection) was administered to mice, and an in vivo PK study was performed. Results: The Cmax value of SR-1277 in mice was 1.2 μM, the Cl value was 2.8 ml/min/kg, the AUC value was 1.26 μM•h, and the half-life was 1.42 h. [1] |
Alias | SR1277 |
Molecular Weight | 477.5 |
Formula | C21H19N9O3S |
Cas No. | 1446715-47-4 |
Smiles | O=[N+](C1=CC=CC2=C1NC(CNC3=NC(N4CCOCC4)=NC5=C3N=CN5C6=CSC=C6)=N2)[O-] |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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