TP-3654

CAS No. 1361951-15-6

TP-3654( TP3654 | TP 3654 )

Catalog No. M11491 CAS No. 1361951-15-6

A potent, selective, orally active second-generation PIM inhibitor with Ki of 5, 42 and 239 nM for Pim1, 2 and 3, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 47 In Stock
10MG 69 In Stock
25MG 138 In Stock
50MG 222 In Stock
100MG 334 In Stock
200MG Get Quote In Stock
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Biological Information

  • Product Name
    TP-3654
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, orally active second-generation PIM inhibitor with Ki of 5, 42 and 239 nM for Pim1, 2 and 3, respectively.
  • 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.
  • 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.
  • Synonyms
    TP3654 | TP 3654
  • Pathway
    JAK/STAT Signaling
  • Target
    Pim
  • Recptor
    Pim-1|Pim-2|Pim-3
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1361951-15-6
  • Formula Weight
    418.4553096
  • Molecular Formula
    C22H25F3N4O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 10 mM
  • SMILES
    OC(C)(C)[C@H]1CC[C@H](NC2=NN3C(C=C2)=NC=C3C4=CC=CC(C(F)(F)F)=C4)CC1
  • Chemical Name
    Cyclohexanemethanol, α,α-dimethyl-4-[[3-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]-, trans-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Foulks JM, et al. Neoplasia. 2014 May;16(5):403-12.
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