Product Details
| Product Name:
TP-3654 |
CAS No.:
1361951-15-6 |
| Purity:
99.95% |
Supply Ability:
10g |
| Release date:
2024/11/13 |
Product Introduction
Bioactivity
| 名稱 | TP-3654 |
| 描述 | TP-3654, a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM). |
| 細(xì)胞實驗 | 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]. |
| 動物實驗 | 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]. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | 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]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (131.43 mM)
|
| 關(guān)鍵字 | inhibit | Pim | Pim kinases | TP 3654 | Inhibitor | TP-3654 | TP3654 |
| 相關(guān)產(chǎn)品 | 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 |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗肝癌化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
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.
You may like
-
CAS:1253799-29-9
$54.00 / 1mg
-
CAS:1150114-62-7
$30.00 / 5mg
-
CAS:898563-00-3
$84.00 / 1mg
Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$1255.00/1mg |
VIP1Y
|
TargetMol Chemicals Inc.
|
2024-10-28 |
|
|
$0.01/1KG |
VIP5Y
|
Career Henan Chemica Co
|
2020-10-28 |
|
|
$0.00/1kg |
VIP5Y
|
Hebei Yanxi Chemical Co., Ltd.
|
2023-08-16 |
United States