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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
Description | SMO-IN-4 (Compound 24) serves as a potent, orally active antagonist of smoothened, exhibiting an IC50 of 24 nM. It demonstrates antitumor activity [1]. |
In vitro | SMO-IN-4 (10 µM) exhibits minimal inhibition across all CYP isoforms and shows low inhibition of hERG (IC 50 = 38 µM) [1]. |
In vivo | In a murine model of medulloblastoma with subcutaneous xenografts in Ptch1 +/- mice, SMO-IN-4 administered orally at 50 mg/kg daily can lead to tumor regression [2]. The pharmacokinetic properties of SMO-IN-4 (Compound 24) are as follows [2]: In mice, a 10 mg/kg oral dose results in an AUC0-24h of 4183 ng·h/mL, Cmax of 4132 ng/mL, half-life of 1.0 hours, and bioavailability of 49%. In rats, the same oral dose yields an AUC0-24h of 5541 ng·h/mL, Cmax of 2180 ng/mL, half-life of 2.3 hours, and bioavailability of 62%. In dogs, a 5 mg/kg oral dose demonstrates an AUC0-24h of 7656 ng·h/mL, Cmax of 1300 ng/mL, half-life of 5.4 hours, and bioavailability of 72%. |
Molecular Weight | 450.96 |
Formula | C24H27ClN6O |
Cas No. | 1567963-99-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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