1125780-41-7 Usage
Biological Activity
sklb610 is a selective inhibitor of vegfr with ic50 value of 2.2 μm [1].vegfr (vascular endothelial growth factor receptor) are receptors for vegf and plays an important role in stimulating cellular response by cooperating with vegf. it has been reported that vegfr abnormally expressed in a variety of cancers and its inhibitors has been regarded as a promising strategy in clinic [1, 2].sklb610 is a potent vegf induced vegf2 phosphorylation inhibitor. when tested with a panel of human cancer cell lines, sklb610 inhibited cell proliferation with ic50 value ranges from 2.2 μm to 25.6 μm. in huvecs, sklb610 showed inhibition on vegf-stimulated cell proliferation as well as vegfr2 phosphorylation, inhibited cell capillary tube formation in a dose-dependent manner [1]. the solubility of sklb610 in water, ethanol, ethyl acetate, 0.5% tween 80 and nanosuspension is 0.34 μg/ml, 16500 μg/ml, 380μg/ml, 23μg/ml and 103μg/ml [2, 3].in mouse model with hct116 subcutaneous xenograft, administration of sklb610 (12.5 mg/kg, 25 mg/kg and 50 mg/kg) for 10 days markedly delayed tumor growth in a concentration dependent manner. further, after 30 days treatment sklb610significantly suppressed tumor volume as 77.1 % at the dose of 50 mg/kg [1].
references
[1]. cao, z.x., et al., sklb610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. cell physiol biochem, 2011. 27(5): p. 565-74.[2]. luo, x., et al., pharmacokinetic studies of a novel multikinase inhibitor for treating cancer by hplc-uv. j chromatogr sci, 2013. 51(1): p. 17-20.[3]. huang, y., et al., the preparation and evaluation of water-soluble sklb610 nanosuspensions with improved bioavailability. aaps pharmscitech, 2013. 14(3): p. 1236-43.
Check Digit Verification of cas no
The CAS Registry Mumber 1125780-41-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,2,5,7,8 and 0 respectively; the second part has 2 digits, 4 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1125780-41:
(9*1)+(8*1)+(7*2)+(6*5)+(5*7)+(4*8)+(3*0)+(2*4)+(1*1)=137
137 % 10 = 7
So 1125780-41-7 is a valid CAS Registry Number.
1125780-41-7Relevant academic research and scientific papers
Synthesis and biological evaluation of novel 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives as potential antitumor agents
Hu, Min,Meng, Nana,Xia, Yong,Xu, Youzhi,Yu, Luoting,Zeng, Xiuxiu,Zhou, Shuyan
, (2021/06/11)
A novel series of 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives were synthesized and evaluated against different tumor cell lines. Experiments in vitro showed that these derivatives could inhibit the proliferation of two kinds of human cancer cell lines (HepG2, HCT116) at low micromolar concentrations and the most potent analog 5q possessed broad-spectrum antiproliferative activity. Experiments in vivo demonstrated that 5q could effectively prolong the longevity of colon carcinoma-burdened mice and slow down the progression of cancer cells by suppression of angiogenesis and the induction of apoptosis and necrosis.
KINASE INHIBITOR COMPOUNDS, COMPOSITIONS, AND METHODS OF TREATING CANCER
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, (2018/03/09)
The present invention relates to a compound having the structure of formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where X, Y, Z, R, R1, R2, R3, R4, R5, and R6 are as described herein. The present invention also relates to compositions containing the compound having the structure of formula (I), and a method of treating cancer in a subject.
