TP-3654

SKU: orb1302789

Description

TP-3654

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1361951-15-6
• MW: 418.46
• Purity: 99.80%
• Formula: C₂₂H₂₅F₃N₄O
• SMILES: CC(C)(O)[C@H]1CC[C@@H](CC1)Nc1ccc2ncc(-c3cccc(c3)C(F)(F)F)n2n1
• Target: Pim
• Solubility: DMSO:55 mg/mL (131.43 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.78 mM)

Bioactivity

• Target IC50:
  Pim2:239 nM (Ki)|Pim3:42 nM (Ki)|Pim1:5 nM (Ki)
• 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.
• 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 .
• 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.
• 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.

Storage & Handling

• Storage: keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, TP 3654, TP3654, TP-3654, Pim2, Pim3, Pim1, Pim, Pim kinases

Compound Identifiers

PubChem CID

66598080