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TP-3654

Catalog No. T4523 CAS 1361951-15-6

TP-3654 is a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM).

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TP-3654, CAS 1361951-15-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 371.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.95%

Purity: 97.72%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TP-3654 is a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM).
Targets&IC50	Pim1:5 nM (Ki), Pim3:42 nM (Ki), Pim2:239 nM (Ki)
In vitro	TP-3654 exhibits strong specificity and activity against PIM-1 in systems overexpressing PIM-1/BAD, achieving an average EC50 of 67 nM. It effectively diminishes phospho-BAD levels in vitro within the UM-UC-3 bladder cancer cell line. Moreover, TP-3654 significantly hampers colony growth in both T24 and UM-UC3 cells, underscoring the reliance of these cell lines on PIM-1 for their proliferation [1].
In vivo	TP-3654 (200 mg/kg, i.g.) significantly reduces both UM-UC-3 and PC-3 tumour growth measured by volume (calliper) and by final tumour weight, with no significant changes in body weight or gross adverse toxicity[1].
Cell Research	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[1].
Animal Research	When tumours of mice reach 100 to 200 mm3 by calliper measurement, mice are randomized and oral dosing of TP-3654 or vehicle control began and continued every day for 5 days with 2 days off for 18 to 21 days. Tumour volumes and body weights were determined twice a week[1].

Molecular Weight	418.46
Formula	C22H25F3N4O
CAS No.	1361951-15-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (131.43 mM)

References and Literature

1. Foulks JM, et al. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Neoplasia. 2014 May;16(5):403-12.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Apoptosis Compound Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library

Related Products

Related compounds with same targets

(2R)-Octyl-α-hydroxyglutarate (Z)-SMI-4a HJ-PI01 SGI-1776 Pim-1 kinase inhibitor 8 AZD1208 Neoprzewaquinone A TCS-PIM-1-4a

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TP-3654 1361951-15-6 Chromatin/Epigenetic JAK/STAT signaling Pim inhibit Pim kinases TP 3654 Inhibitor TP3654 inhibitor

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