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Sitravatinib malate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sitravatinib malate图片
CAS NO:2244864-88-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
MGCD516 malate
MG-516 malate
产品介绍
Sitravatinib malate (MGCD516 malate) 是一种有口服活性的受体酪氨酸激酶 (RTK) 抑制剂。抑制 Axl,MER,VEGFR3,VEGFR2,VEGFR1,KIT,FLT3,DDR2,DDR1,TRKA,和 TRKB,IC50分别为 1.5 nM,2 nM,2 nM,5 nM,6 nM,6 nM,8 nM,0.5 nM,29 nM,5 nM,和 9 nM。Sitravatinib malate 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。
生物活性

Sitravatinib malate (MGCD516 malate) is an orally bioavailablereceptor tyrosine kinase (RTK)inhibitor withIC50s 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[1]. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity ofPD-1blockade through promoting an antitumor immune microenvironment[2].

IC50& Target[1]

VEGFR1

6 nM (IC50)

VEGFR2

5 nM (IC50)

VEGFR3

2 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)

KIT

6 nM (IC50)

FLT3

8 nM (IC50)

体外研究
(In Vitro)

Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines[2].
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[2].

Cell Viability Assay[2]

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
(In Vivo)

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[2].

Animal Model:6-week-old C57BL/6 mice (bearing CT1B-A5 cells)[2]
Dosage:20 mg/kg
Administration:Oral administration; once per day for 6 days
Result:Significantly inhibited tumor progression and induced tumor regression.
Clinical Trial
分子量

763.76

Formula

C37H35F2N5O9S

CAS 号

2244864-88-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.