货号	规格	价格	上海	北京	珠海	重庆	武汉
S82021-5mg买3赠1	≥98%	￥360.00 S82021-5mg ￥360.00 现货（买3赠1）	50 >10	-	-	-	-
S82021-10mg买3赠1	≥98%	￥610.00 S82021-10mg ￥610.00 现货（买3赠1）	25 >10	-	-	-	-
S82021-50mg	≥98%	￥1200.00 S82021-50mg ￥1200.00 现货	5 5	-	-	-	-
S82021-100mg	≥98%	￥2300.00 S82021-100mg ￥2300.00 现货	2 2	-	-	-	-

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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);DiscoidinDomainReceptor(DDR); VEGFR; FLT; Trkreceptor; TAMReceptor; c-Kit; EphrinReceptor

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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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