A Pim kinase inhibitor
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TP-3654

Item No. 29571

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-α,α-dimethyl-4-[[3-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]-cyclohexanemethanol
CAS Number
1361951-15-6
Molecular Formula
C22H25F3N4O
Formula Weight
418.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMSO: 16 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 10 mg/ml
λmax
217, 274, 342 nm
SMILES
CC(C)(O)[C@H]1CC[C@H](NC2=NN3C(C=C2)=NC=C3C4=CC=CC(C(F)(F)F)=C4)CC1
InChi Code
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-
InChi Key
XRNVABDYQLHODA-JCNLHEQBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $63

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    10 mg

    $118

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    25 mg

    $242

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    Product Description

    TP-3654 is an inhibitor of Pim kinases (Kis = 5, 239, and 42 nM for Pim-1, Pim-2, and Pim-3, respectively).1 It inhibits 19 additional kinases, including PI3Kα, PI3Kγ, and PI3Kδ, with IC50 values of less than 300 nM. TP-3654 inhibits phosphorylation of Bad in HEK293 cells overexpressing Bad and Pim-1 (EC50 = 67 nM), as well as in UM-UC-3 cells. It reduces tumor growth in UM-UC-3 bladder carcinoma and PC3 prostate adenocarcinoma mouse xenograft models when administered at a dose of 200 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Foulks, J.M., Carpenter, K.J., Luo, B., et al. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Neoplasia 16(5), 403-412 (2014).