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TP-3654

CAS No. : 1361951-15-6

MCE 站：TP-3654

产品活性：TP-3654是第二代Pim激酶抑制剂，对Pim-1和Pim-3的K_i值分别为5和42 nM。

研究领域：JAK/STAT Signaling

作用靶点：Pim

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.

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  PIM-447 dihydrochloride  |  Pim1/AKK1-IN-1  |  Hispidulin  |  TCS-PIM-1-4a  |  TCS PIM-1 1  |  Quercetagetin  |  M-110  |  SMI-16a  |  CK2/ERK8-IN-1  |  CK2/PIM1-IN-1  |  CX-6258 hydrochloride  |  R8-T198wt

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