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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $297 | In Stock | |
5 mg | $647 | In Stock | |
10 mg | $987 | In Stock | |
25 mg | $1,470 | In Stock | |
50 mg | $1,990 | In Stock | |
100 mg | $2,680 | In Stock |
Description | GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani. |
In vitro | GSK3186899 is active in cidal axenic amastigote assay with an EC50 value of 0.1 μM. GSK3186899 shows good selectivity against mammalian THP-1 host cells (EC50 value > 50 μM). GSK3186899 exhibits a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is more active using human peripheral blood mononuclear cells as the host cells[1]. |
In vivo | In the mouse model of infection, GSK3186899 (25 mg/kg; orally) reduces parasite levels by 99%. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). There are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested[1]. |
Alias | 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide, DDD-853651 |
Molecular Weight | 491.53 |
Formula | C19H28F3N7O3S |
Cas No. | 1972617-87-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 200 mg/mL (406.89 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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