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关于此项目
经验公式(希尔记法):
C19H16ClN3O
化学文摘社编号:
分子量:
337.80
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
SMILES string
Clc1ccc(cc1)NC(=O)c2c(cccc2)NCc3ccncc3
InChI
1S/C19H16ClN3O/c20-15-5-7-16(8-6-15)23-19(24)17-3-1-2-4-18(17)22-13-14-9-11-21-12-10-14/h1-12,22H,13H2,(H,23,24)
InChI key
GGPZCOONYBPZEW-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 5 mg/mL, methanol: soluble
shipped in
wet ice
storage temp.
−20°C
Quality Level
General description
A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC50 = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC50 = 7.0 µM and 7.3 µM). Also displays antiangiogenic and antitumor properties. Does not inhibit the activities of CDK-1, c-Met, IGF-1R or PKA (IC50 >10 µM).
A pyridinyl-anthranilamide compound that displays both antiangiogenic and antitumor properties. A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC50 = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC50 = 7 µM and 7.3 µM). Further, inactive towards the inhibition of CDK-1, c-Met, IGF-1R and PKA (IC50 >10 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Kinase activities of KDR, Flt-1 and c-Kit
Kinase activities of KDR, Flt-1 and c-Kit
Product competes with ATP.
Reversible: yes
Target IC50: 20 nM, 180 nM and 240 nM against kinase activities of KDR, Flt-1 and c-Kit, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Furet, P., et al. 2003. Bioorg. Med. Chem. Lett.13, 2967.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Shu-Yun Li et al.
Biology of reproduction, 105(4), 958-975 (2021-05-20)
Testis differentiation is initiated when Sry in pre-Sertoli cells directs the gonad toward a male-specific fate. Sertoli cells are essential for testis development, but cell types within the interstitial compartment, such as immune and endothelial cells, are also critical for
Perivascular cells support folliculogenesis in the developing ovary.
Li, et al.
Proceedings of the National Academy of Sciences of the USA, 119, e2213026119-e2213026119 (2023)
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