796967-16-3 Usage
Chemical Properties
Beige Solid
Uses
Different sources of media describe the Uses of 796967-16-3 differently. You can refer to the following data:
1. Linifanib (ABT-869) is a novel, potent ATP-competitive RTK inhibitor for KDR, CSF-1R, Flt-1, Flt-3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM, 3 nM, and 66 nM respectively.
2. Linifanib (ABT 869) is an oral tyrosine kinase inhibitor with antineoplasic activity. As a dual inhibitor, Linifanib, is being tested on several different cancers.
3. An oral tyrosine kinase inhibitor with antineoplasic activity.
Definition
ChEBI: A member of the class of ureas that is urea in which one of the nitrogens is substituted by a 2-fluoro-5-methylphenyl group, while the other nitrogen is substituted by a p-(3-amino-1H-indazol-4-yl)phenyl group. It is a poten
, selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinases.
Biological Activity
linifanib (abt-869) is an effective atp-competitive tyrosine kinase inhibitor against the platelet-derived growth factor (pdgf) receptor and the vascular endothelial growth factor receptor (vegfr) families, including constitutively active fms-like receptor tyrosine kinase 3 (flt3) [1][2]. it is of ic50 values of 0.55 nmol/l and 6 μmol/l to the cell growth in ba/f3 flt3 itd mutant cells and in ba/f3 flt3 wt cells, respectively [1].flt3 is important in controlling the proliferation and differentiation of hematopoietic cells. patients with acute myeloid leukemia (aml) showed activating mutations in flt3. these mutations caused abnormal cell proliferation [1].linifanib at a concentration of 10 nmol/l induced apoptosis in internal tandem duplication (itd) mutant cells, but showed no effect in wt cells. treatment with linifanib did not differentiate wt cells from flt3 mutant cells with mutation at d835v, in inhibiting proliferation or reducing cell viability. in ba/f3 flt3 itd cell lines, linifanib at a concentration of 10 nmol/l, effectively inhibited the phosphorylation of flt3. 10 nmol/l linifanib reduced the phosphorylation of akt at ser473 [1].daily orally treatment with linifanib by gavage in nod/scid mice with itd mutant cell decreased the leukemia progression rate compared with the control. on day 7, itd mutant cells showed rapid progression in control mice, whereas linifanib-treated mice showed no detectable disease. in addition, daily linifanib-treated mice with itd mutant cells showed significantly longer (p < 0.01) survival duration than control mice with itd mutant cells only [1].
references
[1]. jenny e. hernandez-davies, joan p. zape, elliot m. landaw, et al. the multitargeted receptor tyrosine kinase inhibitor linifanib (abt-869) induces apoptosis through an akt and glycogen synthase kinase 3β–dependent pathway. mol. cancer ther., 2011, 10(6):949-59.[2]. joyce e. ohm, michael r. shurin, clemens esche, et al. effect of vascular endothelial growth factor and flt3 ligand on dendritic cell generation in vivo. journal of immunology, 1999, 163:3260-3268.
Check Digit Verification of cas no
The CAS Registry Mumber 796967-16-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,9,6,9,6 and 7 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 796967-16:
(8*7)+(7*9)+(6*6)+(5*9)+(4*6)+(3*7)+(2*1)+(1*6)=253
253 % 10 = 3
So 796967-16-3 is a valid CAS Registry Number.
InChI:InChI=1/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28)
796967-16-3Relevant articles and documents
N - (4 - (3 - amino - 1 H - indazole - 4 - yl) phenyl) - N' - (2 - fluoro - 5 - methylphenyl) urea intermediate preparation method
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, (2018/03/02)
The invention provides a preparation method of N-(4-(3-amino-1H-indazol-4-yl) phenyl)-N'-(2-fluoro-5-methylphenyl) urea and an intermediate thereof. Specifically, the invention provides a preparation method of a borate ester compound as shown in a formula I, and the preparation method comprises the following steps: enabling a compound as shown in a formula III to react with a compound as shown in a formula IV to generate a compound as shown in a formula V, and enabling the compound as shown in the formula V to react with a boron reagent to generate the compound as shown in the formula I. The method has the characteristics of convenience in reaction, easiness in obtainment of the intermediate, high yield, high product purity of above 98.5%, low cost of raw materials and the like, and is suitable for industrial application.
The discovery and development of a safe, practical synthesis of ABT-869
Kruger, Albert W.,Rozema, Michael J.,Chu-Kung, Alexander,Gandarilla, Jorge,Haight, Anthony R.,Kotecki, Brian J.,Richter, Steven M.,Schwartz, Albert M.,Wang, Zhe
experimental part, p. 1419 - 1425 (2010/04/22)
The discovery, development and implementation of two chemical routes to ABT-869 is reported. Optimization of the first-generation heterocycle formation and Suzuki coupling is briefly described. Key features of the second-generation synthesis include the development of a safe hydrazine condensation by utilizing an inorganic base to increase the onset temperature of exothermic decomposition. The second-generation Suzuki reaction is discussed in detail, culminating in the use of an oxygen monitor as a PAT to maximize reproducibility on scale.
CRYSTALLINE CHEMOTHERAPEUTIC
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Page/Page column 13, (2009/05/28)
N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.
