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编 号：F040833
分子式：C33H29F2N5O4S
分子量：629.68
分子式：C33H29F2N5O4S
分子量：629.68
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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200mg
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CAS No: 1123837-84-2
产品详情
生物活性：
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.
体内研究：
Sitravatinib (20 mg/kg；口服；每天一次，持续 6 天) 在携带 CT1B-A5 细胞模型的 C57BL/6 小鼠中显着抑制肿瘤进展并诱导肿瘤消退。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.
体外研究：
Sitravatinib (0.01 nM-10 μM；14 天) 在 KLN205 和 E0771 细胞系中以剂量依赖性方式减少集落形成。 Sitravatinib (0.001-10 μM；5 天) 在 KLN205、E0771 和 CT1B-A5 细胞系中抑制肿瘤细胞活力，IC50 约为 1 μM。
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.
体内研究：
Sitravatinib (20 mg/kg；口服；每天一次，持续 6 天) 在携带 CT1B-A5 细胞模型的 C57BL/6 小鼠中显着抑制肿瘤进展并诱导肿瘤消退。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.
体外研究：
Sitravatinib (0.01 nM-10 μM；14 天) 在 KLN205 和 E0771 细胞系中以剂量依赖性方式减少集落形成。 Sitravatinib (0.001-10 μM；5 天) 在 KLN205、E0771 和 CT1B-A5 细胞系中抑制肿瘤细胞活力，IC50 约为 1 μM。
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