Product Details
| Product Name:
Entospletinib |
CAS No.:
1229208-44-9 |
| Purity:
99.51% |
Supply Ability:
10g |
| Release date:
2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Entospletinib |
| 描述 | Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable. |
| 細(xì)胞實(shí)驗(yàn) | In MV-4-11 cells, the functional effect of the compound on the cellular Flt3 activity was determined by inhibition of cell proliferation. Cells were diluted in 96 well flat bottom tissue culture plates in RPMI medium containing 10% FBS and compound dilutions were added and incubated at 37°C for 72 hours. Aramazol (10%) was added to the cells and the cells were incubated for another 12-18 hours at 37°C. Finally, the inhibition of the relative cell number was measured at 570/600 nm in the spectrophotometer. |
| 激酶實(shí)驗(yàn) | In the determination of full-length baculovirus expressed Syk kinase activity, the reaction system was 25 μL containing 25 mM Tris-HCl, pH 7.5, 5 mM β-glycerophosphate, 2 mM DTT, 0.1 mM Na3VO4, 10 mM MgCl2, 0.5 μM Promega PTK Biotin Peptide Substrate 1, 0.01% casein, 1, 0.01% Triton X-100, 0.25% Glycerol, and 40 mM ATP (Km for ATP). After incubation for 60 minutes at room temperature, the reaction was stopped by adding 30 mM EDTA (30 μL of SA-APC and 4 nM PT-66 antibody). After measuring the plate, the IC50 value of the test compound was calculated using a 4-parameter linear regression algorithm. |
| 動(dòng)物實(shí)驗(yàn) | In the rat collagen-induced arthritis (CIA) model, Entospletinib (10 mg/kg), which is dissolved in hydrogenated castor oil,ethanol or physiological saline, is taken by oral. |
| 體外活性 | In cells, GS-9973 also displays excellent specificity for Syk, and effectively inhibits BCR-mediated activation and proliferation of B-cells, as well as immune-complex-stimulated cytokine production in monocytes. In Caco-2 cell, GS-9973 exhibits good bidirectional permeability across cell monolayers. |
| 體內(nèi)活性 | In rat and dog, Entospletinib (1 mg/kg) by oral administration shows moderate to high bioavailability. In a rat collagen-induced arthritis model, Entospletinib (1-10 mg/kg) by oral administrations significantly suppress ankle inflammation. Entospletinib(ED50 =1.2 -3.9 mg/kg) exhibits disease-modifying activity such as pannus formation, cartilage damage, bone resorption, and periosteal bone formation. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (121.52 mM)
|
| 關(guān)鍵字 | Syk | inhibit | Spleen tyrosine kinase | Entospletinib | GS 9973 | GS9973 | Inhibitor |
| 相關(guān)產(chǎn)品 | Fostamatinib | R112 | Syk-IN-3 | Ellagic acid | Piceatannol | Cerdulatinib | PRT062607 hydrochloride | Fostamatinib Disodium | ANTHRAQUINONE-2-CARBOXYLIC ACID | GSK1904529A | Cerdulatinib hydrochloride | R406 free base |
| 相關(guān)庫(kù) | 酪氨酸激酶分子庫(kù) | 激酶抑制劑庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 抗癌上市藥物庫(kù) | FDA 上市激酶抑制劑庫(kù) | 已知活性化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(kù) |
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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United States