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  • DC Chemicals Limited
  • China
  • Product Name: TP-3654
  • Price: $550.0/100mg $1000.0/250mg $1900.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1361951-15-6

1361951-15-6 structure
1361951-15-6 structure
  • Name: TP-3654
  • Chemical Name: TP-3654
  • CAS Number: 1361951-15-6
  • Molecular Formula: C22H25F3N4O
  • Molecular Weight: 418.464
  • Catalog: Signaling Pathways JAK/STAT Signaling Pim
  • Create Date: 2018-04-25 02:19:57
  • Modify Date: 2024-01-02 17:35:05
  • TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.

Name TP-3654
Synonyms 2-[4-[[3-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]cyclohexyl]propan-2-ol
Description TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
Related Catalog
Target

Ki: 5 nm(Pim-1), 239 nM (Pim-2), 42 nM (Pim-3)[1]

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[1].
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[1].
Cell Assay 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 Admin When tumors of mice reaches 100 to 200 mm3 by caliper 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. Tumor volumes and body weights were determined twice a week[1].
References

[1]. Foulks JM, et al. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Neoplasia. 2014 May;16(5):403-12.

Molecular Formula C22H25F3N4O
Molecular Weight 418.464
Storage condition 2-8℃