| Name | TP-3654 |
| Description | TP-3654, a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM). |
| Cell Research | 1 μM TP-3654 is tested against 336 kinases at a concentration of 10 μM ATP. IC50 determinations of phosphoinositide 3-kinase (PI3K) (α, β, δ, and γ) and all kinases inhibited by >50% from the initial screen are performed using 10-dose, three-fold serial dilutions of TP-3654 starting with 10 μM at Km ATP concentrations for each kinase[1]. |
| Animal Research | When tumours of mice reach 100 to 200 mm3 by calliper measurement, mice are randomized and oral dosing of TP-3654 or vehicle control began and continued every day for 5 days with 2 days off for 18 to 21 days. Tumour volumes and body weights were determined twice a week[1]. |
| In vitro | TP-3654 exhibits strong specificity and activity against PIM-1 in systems overexpressing PIM-1/BAD, achieving an average EC50 of 67 nM. It effectively diminishes phospho-BAD levels in vitro within the UM-UC-3 bladder cancer cell line. Moreover, TP-3654 significantly hampers colony growth in both T24 and UM-UC3 cells, underscoring the reliance of these cell lines on PIM-1 for their proliferation [1]. |
| In vivo | TP-3654 (200 mg/kg, i.g.) significantly reduces both UM-UC-3 and PC-3 tumour growth measured by volume (calliper) and by final tumour weight, with no significant changes in body weight or gross adverse toxicity[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (131.43 mM)
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| Keywords | inhibit | Pim | Pim kinases | TP 3654 | Inhibitor | TP-3654 | TP3654 |
| Inhibitors Related | XL413 hydrochloride | HJ-PI01 | SGI-1776 | CK2/ERK8-IN-1 | M-110 | (Z)-SMI-4a | XL413 HCl | CX-6258 hydrochloride | Pim-1 kinase inhibitor 4 | Pim-1/2 kinase inhibitor 1 | Pim-1 kinase inhibitor 8 | K00135 |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
