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Linifanib

CAT: 0013-GTR19161902-02Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161902-02Size:5 mg
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Description
A potent multi-RTKs inhibitor of members of VEGFR and PDGFR families with IC50 of 4/3/3/14/4/66/190/170 nM for KDR/FLT1/CSF1R/KIT/FLT3/PDGFRβ/FLT4/Tie2, respectively; much less active (IC50>10 uM) against other nonrelated tyrosine kinases, such as steroid receptor coactivator and EGFR; inhibits RTK phosphorylation (IC50=2, 4, and 7 nM for PDGFRβ, KDR, and CSF-1R, respectively) and VEGF-stimulated proliferation (IC50=0.2 nM for human endothelial cells) ; exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models (ED50=1.5-5 mg/kg, twice daily) .Colon Cancer Phase 2 Discontinued (In Vitro) :Linifanib (0-10000 nM; 72 hours) inhibits in vitro the cell proliferation of 8305C and 8505C cell lines in a concentration-dependent manner.Linifanib significantly decreased the levels of phospho-CSF-1R after 24 h and 72 h in both 8505C and 8305C cells. (In Vivo) :The synergistic ATC antitumor activity of linifanib (10 mg/kg; p.o.; daily for 33 days) /Irinotecan combination significantly increases the survival of ATC affected mice and induces some complete responses.
CAS Number
796967-16-3
Product Name Alternative
ABT-869 | AL-39324 | ABT 869 | ABT869 | AL 39324 | AL39324
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=C (N) N (C1=CC=C (C2=CC=CC3=C2C (N) =NN3) C=C1) C4=CC (C) =CC=C4F
Molecular Formula
C21H18FN5O
Molecular Weight
375.3989
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Urea, N-[4- (3-amino-1H-indazol-4-yl) phenyl]-N'- (2-fluoro-5-methylphenyl) -

Chemical Information

Linifanib

Linifanib is a member of the class of phenylureas that is urea in which one of the nitrogens is substituted by a 2-fluoro-5-methylphenyl group, while the other is substituted by a p-(3-amino-1H-indazol-4-yl)phenyl group. It is a potent, selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinases. It has a role as an antineoplastic agent, an angiogenesis inhibitor and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a member of phenylureas, an aromatic amine and a member of indazoles.

CAS Number796967-16-3
PubChem CID11485656
IUPAC Name1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea
Molecular FormulaC21H18FN5O
Molecular Weight375.4
XLogP3.9
Topological Polar Surface Area95.8
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Heavy Atom Count28
Formal Charge0
Complexity541
SMILES
CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N
InChI
InChI=1S/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)
InChIKey
MPVGZUGXCQEXTM-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Linifanib
CAS: 796967-16-3
CID: 11485656
Formula: C21H18FN5O
MW: 375.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight375.4
XLogP33.9
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Exact Mass375.14953838
Monoisotopic Mass375.14953838
Topological Polar Surface Area95.8 Ų
Heavy Atom Count28
Formal Charge0
Complexity541
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
015580Linifanib
HY-50751G-01Linifanib (GMP)
HY-50751SLinifanib-d4
HY-50751RLinifanib (Standard)
SF5368-5mgLinifanib (VEGFR inhibitor)
E1KS1003Linifanib (ABT-869)

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