Product Details
| Product Name:
Sitravatinib |
CAS No.:
1123837-84-2 |
| Purity:
99.74% |
Supply Ability:
10g |
| Release date:
2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | Sitravatinib |
| 描述 | Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl. |
| 細(xì)胞實(shí)驗(yàn) | Cell lines: DDLS,LS141,and MPNST. Concentrations: 62.5,125,250,500,1000,2000 nM2,000-3,000 cells were plated in 96-well plates in RPMI/DME media with 10% FBS and then treated with the indicated drugs the next day.After 72 hours,media was replaced with 100 μL of media with 10% serum and 10% CCK-8 solution.After 1 hour,the optical density was read at 450 nm to determine viability.Background values from negative control wells without cells were subtracted for final sample quantification.Data was plotted as % cell viability compared to DMSO control. |
| 動(dòng)物實(shí)驗(yàn) | Animal Models: ICR/SCID mice. Formulation: 0.5% hydroxypropyl methylcellulose (HPMC) and 0.1% Tween-80 solution (pH 1.4). Dosages: 15 mg/kg. Administration: p.o. |
| 體外活性 | Sitravatinib (MGCD516) is an inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (PDGFR, VEGFR, and KIT), DDR2, TRK family, MET, and AXL. Sitravatinib causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. |
| 體內(nèi)活性 | Sitravatinib (MGCD516) has antitumor activity in nonClinicalal cancer models harboring genetic alterations of sitravatinib targets, including the rearrangement of NTRK, RET, or CHR4q12 amplification. In vivo tumor xenografts, MGCD516 causes the significant suppression of tumor growth. Efficacy of MGCD516 is superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo. |
| 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 (79.41 mM)
|
| 關(guān)鍵字 | RTK | PD-1 | SCFR | DDR1 | inhibit | VEGFR2 | MER | immune | TRKA | Cluster of differentiation antigen 135 | Cancer | Discoidin Domain Receptor | VEGFR3 | Inhibitor | Vascular endothelial growth factor receptor | Trk Receptor | Tropomyosin related kinase receptor | CD135 | MGCD 516 | VEGFR | immunotherapy | Macrophages | MG-516 | c-Kit | MGCD-516 | DDR2 | VEGFR1 | Tyrosine | Sitravatinib | MG 516 | Fms like tyrosine kinase 3 | FLT3 | Axl | TRKB | KIT | kinase | CD117 |
| 相關(guān)產(chǎn)品 | Ribociclib | Gilteritinib | Nintedanib | Regorafenib monohydrate | Sorafenib | Pexidartinib | Regorafenib | Amitriptyline hydrochloride | Sorafenib tosylate | Imatinib | Pazopanib | Axitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(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) | 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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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$2500.00/100mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-10-23 |
United States