TP-3654

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性、口服活性的第二代 PIM 抑制剂，对 Pim1、2 和 3 的 Ki 值分别为 5、42 和 239 nM。

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.

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.

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.

TP3654 | TP 3654

JAK/STAT Signaling

Pim

Pim-1|Pim-2|Pim-3

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1361951-15-6

418.4553096

C22H25F3N4O

>98% (HPLC)

DMSO: 10 mM

OC(C)(C)[C@H]1CC[C@H](NC2=NN3C(C=C2)=NC=C3C4=CC=CC(C(F)(F)F)=C4)CC1

Cyclohexanemethanol, α,α-dimethyl-4-[[3-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazin-6-yl]amino]-, trans-

(-20℃)

With Ice Pack

≥ 2 years