Product Details
| Product Name:
TP-3654 |
CAS No.:
1361951-15-6 |
| Purity:
99.95% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | TP-3654 |
| Description | TP-3654, a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM). |
| 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]. |
| 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]. |
| 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)
|
| Keywords | inhibit | Pim | Pim kinases | TP 3654 | Inhibitor | TP-3654 | TP3654 |
| Inhibitors Related | XL413 hydrochloride | HJ-PI01 | SGI-1776 | CK2/ERK8-IN-1 | M-110 | (Z)-SMI-4a | XL413 HCl | CX-6258 hydrochloride | Pim-1 kinase inhibitor 4 | Pim-1/2 kinase inhibitor 1 | Pim-1 kinase inhibitor 8 | K00135 |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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