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TP-3654
Catalog No. T4523Cas No. 1361951-15-6
TP-3654, a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM).
TP-3654
Catalog No. T4523Cas No. 1361951-15-6
TP-3654, a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $52 | In Stock | |
| 10 mg | $77 | In Stock | |
| 25 mg | $153 | In Stock | |
| 50 mg | $247 | In Stock | |
| 100 mg | $371 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $52 | In Stock |
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Purity:99.95%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | TP-3654, a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM). |
| Targets&IC50 | Pim3:42 nM (Ki), Pim1:5 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (131.43 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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