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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 |
| Related Pim Products |
|---|
| SGI-1776
SGI-1776 is novel small molecule inhibitor of PIM kinase activity with IC50 of 7 ± 1.8, 363 ± 27.6 and 69 ± 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively. |
| SMI-4a
SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modest potent to Pim-2, does not significantly inhibit other serine/threonine- or tyrosine-kinases. |
| CX-6258
CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity. |
| TCS PIM-1 1
TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s > 20,000 nM). |
| Hispidulin
Hispidulin is a natural flavonoid with a wide range of biological activities. Hispidulin is an inhibitor of PIM-1 with IC50 value of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. |
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