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Enpp-1-IN-12 (compound 43), an orally active and potent inhibitor of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) with a K_i of 41 nM, exhibits anti-tumor activity [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | 1.444 € | 10-14 weeks | |
50 mg | 1.881 € | 10-14 weeks | |
100 mg | 2.375 € | 10-14 weeks |
Description | Enpp-1-IN-12 (compound 43), an orally active and potent inhibitor of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) with a K_i of 41 nM, exhibits anti-tumor activity [1]. |
In vitro | Enpp-1-IN-12 (5 μM) exhibits a half-life of over 120 minutes and an intrinsic clearance rate below 11.55 μL/min/million cells in human hepatocytes, compared to a half-life of 61.88 minutes and a clearance rate of 22.4 μL/min/million cells in mouse hepatocytes [1]. |
In vivo | Enpp-1-IN-12, at a dosage of 100 mg/kg administered orally, effectively inhibits tumor growth in a syngeneic murine model for lung cancer derived from LLC1 cells. At a lower dose of 10 mg/kg, the compound demonstrates moderate oral bioavailability (F=45.1%) with a half-life of 1.04 hours and a peak concentration (C max) of 303.10 ng/mL in healthy female BALB/c mice. When administered intravenously at 1 mg/kg, Enpp-1-IN-12 shows a half-life of 0.76 hours, a peak concentration of 308.64 ng/mL, and a clearance rate of 73.22 mL/min/kg in the same mouse model. |
Molecular Weight | 373.43 |
Formula | C17H19N5O3S |
Storage | Shipping with blue ice. |
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