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Chromatin/Epigenetic Pim TP-3654

TP-3654

Catalog No. T4523   CAS 1361951-15-6
Synonyms: TP3654, TP 3654,
Purity 99.95% Datasheet

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

TP-3654, CAS 1361951-15-6
Pack Size Availability Price/USD Quantity
5 mg In stock 58.00
10 mg In stock 86.00
25 mg In stock 172.00
50 mg In stock 275.00
100 mg In stock 413.00
1 mL * 10 mM (in DMSO) In stock 58.00
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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 Pim-1 :ic50 5 nM (Ki),   Pim-2 :ic50 239 nM (Ki),   Pim-3 :ic50 42 nM (Ki),  
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].

Description

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

Targets&IC50

Pim-1 :ic50 5 nM (Ki)

Pim-2 :ic50 239 nM (Ki)

Pim-3 :ic50 42 nM (Ki)

In Vitro

TP-3654 shows 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 [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].

Synonyms TP3654, TP 3654,
Purity 99.95%
Appearance solid
Molecular Weight 418.46
Formula C22H25F3N4O
CAS No. 1361951-15-6

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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:
Bioactive Compound Library Anti-cancer Compound Library Clinical Compound Library Anti-cancer Clinical Compound Library

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Related compounds with same targets
TCS PIM-1 1 AZD1208 SMI-4a SGI-1776 free base SMI-16a SMI-4a CX-6258 HCl XL413 hydrochloride

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