TP-3654

SKU: orb1226449

Description

A potent, selective, orally active second-generation PIM inhibitor with Ki of 5, 42 and 239 nM for Pim1, 2 and 3, respectively; exhibits submicromolar activity in UM-UC-3 bladder cancer cell line; displays favorabl hERG and CYP450 inhibition profiles compared with SGI-1776, reduces tumor growth in vivo xenografts.(In Vitro):TP-3654 demonstrates potent PIM-1 specific cellular activity in the PIM-1/BAD overexpression system with an average EC50 of 67 nM. TP-3654 treatment reduces levels of phospho-BAD in vitro using the bladder cancer cell line UM-UC-3. TP-3654 reduces colony growth of T24 and UM-UC3 cells, confirming the PIM-1–dependent growth for both cell lines.(In Vivo):Oral dosing of 200 mg/kg TP-3654 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.

Key Properties

• CAS Number: 1361951-15-6
• MW: 418.4553096
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₅F₃N₄O
• SMILES: OC(C)(C)[C@H]1CC[C@H](NC2=NN3C(C=C2)=NC=C3C4=CC=CC(C(F)(F)F)=C4)CC1
• Target: Pim
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  Oral dosing of 200 mg/kg TP-3654 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.
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• In Vitro:
  TP-3654 demonstrates potent PIM-1 specific cellular activity in the PIM-1/BAD overexpression system with an average EC50 of 67 nM. TP-3654 treatment reduces levels of phospho-BAD in vitro using the bladder cancer cell line UM-UC-3. TP-3654 reduces colony growth of T24 and UM-UC3 cells, confirming the PIM-1-dependent growth for both cell lines.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TP3654 | TP 3654

Quick Database Links

Gene Symbol

Pim