Sitravatinib
作者：齐岳
发布时间：2023-08-23
09:36:19
点击数：
产品名称：Sitravatinib
产品描述：
| 产品描述 | Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl. |
| 靶点活性 | DDR2:0.5 nM, EPHA3:1 nM, Mer:2 nM, VEGFR3 (FLT4):2 nM, Axl:1.5 nM |
| 体外活性 | MGCD516 (Sitravatinib) 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. MGCD516 causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro. |
| 体内活性 | Sitravatinib 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. |
| 细胞实验 | 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. |
| 动物实验 | 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. |
| 别名 | MG516, MGCD516 |
| 分子量 | 629.68 |
| 分子式 | C33H29F2N5O4S |
| CAS No. | 1123837-84-2 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 32 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
