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• 产品描述： Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment

• 靶点： VEGFR3:2 nM (IC50);VEGFR1:6 nM (IC50);VEGFR2:5 nM (IC50);TrkA:5 nM (IC50);TrkB:9 nM (IC50);DDR1:29 nM (IC50);DDR2:0.5 nM (IC50);Axl:1.5 nM (IC50);MER:2 nM (IC50);FLT3:8 nM (IC50);KIT:6 nM (IC50)

• 体外研究：
  Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines. Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines. Cell Viability Assay Cell Line: KLN205, E0771, CT1B-A5 cells Concentration: 0.001, 0.01, 0.1, 1, 10 μM Incubation Time: 5 days Result: Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM.

• 体内研究：
  Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model. Animal Model: 6-week-old C57BL/6 mice (bearing CT1B-A5 cells) Dosage: 20 mg/kg Administration: Oral administration; once per day for 6 days Result: Significantly inhibited tumor progression and induced tumor regression.

• 参考文献：
  1. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109. 2. Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21). pii: 124184.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.588 ml	7.941 ml	15.881 ml
  5 mM	0.318 ml	1.588 ml	3.176 ml
  10 mM	0.159 ml	0.794 ml	1.588 ml
  50 mM	0.032 ml	0.159 ml	0.318 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *