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.
Product information
CAS Number: 1361951-15-6
Molecular Weight: 418.46
Formula: C22H25F3N4O
Chemical Name: 2-[(1r,4r)-4-({3-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazin-6-yl}amino)cyclohexyl]propan-2-ol
Smiles: CC(C)(O)[C@@H]1CC[C@H](CC1)NC1C=CC2=NC=C(C3=CC=CC(=C3)C(F)(F)F)N2N=1
InChiKey: XRNVABDYQLHODA-JCNLHEQBSA-N
InChi: InChI=1S/C22H25F3N4O/c1-21(2,30)15-6-8-17(9-7-15)27-19-10-11-20-26-13-18(29(20)28-19)14-4-3-5-16(12-14)22(23,24)25/h3-5,10-13,15,17,30H,6-9H2,1-2H3,(H,27,28)/t15-,17-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (119.49 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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