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TP-3654 is a second-generation Pim kinase inhibitor, with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively. TP-3654 demonstrates potent PIM-1 specific cellular activity in the PIM-1/BAD overexpression system with an average EC50 of 67 nM.
In vivo, TP-3654 (200 mg/kg; Oral) significantly reduces both UM-UC-3 and PC-3 tumor growth measured by volume (caliper) and by final tumor weight, with no significant changes in body weight or gross adverse toxicity.
Molecular Weight | 418.46 |
Formula | C22H25F3N4O |
CAS Number | 1361951-15-6 |
Solubility (25°C) | DMSO ≥ 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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