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TP-3654
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TP-3654图片
CAS NO:1361951-15-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 418.46
Formula C22H25F3N4O
CAS No. 1361951-15-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) OC(C)(C)[C@H]1CC[C@H](NC2=NN3C(C=C2)=NC=C3C4=CC=CC(C(F)(F)F)=C4)CC1
Synonyms TP-3654; TP3654; TP 3654
实验参考方法
In Vitro

In vitro activity: TP-3654 is a novel and potent inhibitor of Pim-1 and Pim-3 ( proviral integration site for moloney murine leukemia virus) kinase that is potentially useful for the treatment of various cancers such as prostate cancer, acute myeloid leukemia, multiple sclerosis and psoriasis. As a second-generation PIM inhibitor, TP-3654 displays submicromolar activity in pharmacodynamic biomarker modulation, cell proliferation studies, and colony formation assays using the UM-UC-3 bladder cancer cell line. TP-3654 demostrates favorable human ether-à-go-go-related gene and cytochrome P450 inhibition profiles compared with the first-generation PIM inhibitor, SGI-1776, and exhibits oral bioavailability. In vivo xenograft studies using a bladder cancer cell line show that PIM kinase inhibition can reduce tumor growth, suggesting that PIM kinase inhibitors may be active in human urothelial carcinomas.


Kinase Assay: TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.


Cell Assay: TP-3654 displays submicromolar activity in pharmacodynamic biomarker modulation, cell proliferation studies, and colony formation assays using the UM-UC-3 bladder cancer cell line. TP-3654 demostrates favorable human ether-à-go-go-related gene and cytochrome P450 inhibition profiles compared with the first-generation PIM inhibitor, SGI-1776, and exhibits oral bioavailability. 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

In Vivo In vivo xenograft studies using a bladder cancer cell line show that PIM kinase inhibition can reduce tumor growth, suggesting that PIM kinase inhibitors may be active in human urothelial carcinomas.
Animal model Mice with bladder cancer xenograft model
Formulation & Dosage 200 mg/kg; oral
References Neoplasia. 2014 May;16(5):403-12.