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Enzymes for Research, Diagnostic and Industrial Use

Linifanib (ABT-869)

Cat No.
CEI-0159
Description
As a structurally novel, receptor tyrosine kinase (RTK) inhibitor, ABT-869 can inhibit PDGFR-beta, KDR, and CSF-1R with IC50 of 2 nM, 4 nM and 7 nM.
Alias
AL-39324
CAS No.
796967-16-3
Molecular Weight
375.405
Purity
>99%
Storage
2 years at -20 centigrade
Synonyms
AL-39324
Targets
KDR, CSF-1R, Flt-1, Flt-3, PDGFR-beta
Molecular Formula
C21H18FN5O
Chemical Name
1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea
Solubility
DMSO 75 mg/mL Water
In vitro
As a structurally novel, receptor tyrosine kinase (RTK) inhibitor, ABT-869 can inhibit PDGFR-beta, KDR, and CSF-1R with IC50 of 2 nM, 4 nM and 7 nM. ABT-869 is competitive with ATP, with Ki values of 3 nM and 120 nM. For cell lines (1) MV-4-11 and MOLM-13 cell lines ABT-869, a multitargeted receptor tyrosine kinase inhibitor, inhibited the phosphorylation of FLT3, STAT5, and ERK, as well as Pim-1 expression in MV-4-11 and MOLM-13 cells with IC50 from 1 nM to 10 nM. ABT-869 inhibited the proliferation of MV-4-11 and MOLM-13 with IC50 of 4 nM and 6 nM through the induction of apoptosis by increasing sub-G(0)/G(1) phase, caspase activation, and PARP cleavage. (2)ABT-869 can also inhibit VEGF-stimulated proliferation of human endothelial cells with IC50 of 0.2 nM. (3) In normal human blood spiked with AML cells, ABT-869 inhibited phosphorylation of FLT3 with IC50 approximately 100 nM. (4) ABT-869 had no significant effect up to 1000 nM on normal hematopoietic progenitor cells, whereas in AML patient samples harboring both FLT3-ITD and wt-FLT3, ABT-869 inhibited colony formation with IC50 of 100 and 1000 nM, respectively.
In vivo
ABT-869 exhibits efficacy in human fibrosarcoma and breast, colon, and small cell lung carcinoma xenograft models and is also effective in orthotopic breast and glioma models. ABT-869 can reduce tumor size and tumor regression was observed in epidermoid carcinoma and leukemia xenograft models.
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