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Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 217 | 现货 | |
5 mg | ¥ 477 | 现货 | |
10 mg | ¥ 745 | 现货 | |
25 mg | ¥ 1,390 | 现货 | |
50 mg | ¥ 2,230 | 现货 | |
100 mg | ¥ 3,570 | 现货 | |
200 mg | ¥ 5,190 | 现货 | |
500 mg | ¥ 7,920 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 686 | 现货 |
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) 是一种针对紧密相关RTKs谱系的抑制剂,包括RET、分裂型RTKs(PDGFR、VEGFR和KIT)、DDR2、TRK家族、MET和AXL。MGCD516显著阻断潜在驱动RTKs的磷酸化作用,并在体外实验中引发强大的抗增殖效果。 |
体内活性 | Sitravatinib在含有Sitravatinib靶点遗传变化的非临床癌症模型中展示了抗肿瘤活性,包括NTRK重排、RET重排或CHR4q12扩增。在活体内肿瘤异种移植模型中,MGCD516显著抑制了肿瘤生长。与两种已广泛研究、靶点特异性重叠的多激酶抑制剂imatinib和crizotinib相比,MGCD516在体外及体内的疗效更为卓越。 |
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 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (79.41 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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