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ABT-869 (Linifanib) | KDR, CSF-1R, FLT1/3, PDGFRb inhibitor

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Price:
$129.00
Catalog #:
C2869-5
Quantity:


Product Description

ABT-869 (Linifanib) is an aminobenzopyrazole-based, orally available, ATP-competitive receptor tyrosine kinase inhibitor with IC50 potency against KDR, FLT1, CSF-1R, FLT3, and PDGFRb of 4 nM, 3 nM, 3 nM, 4 nM, and 66 nM, respectively. It is highly selective (> 1uM) against unrelated tyrosine kinases and serine/threonine kinases. [1] In cellular assays, ABT-689 exhibited potency against ligand-induced PDGFRbeat, KIT, and CSF-1R phosphorylation, with IC50s of 2, 31, and 10 nM, respectively.

In vivo, ABT-869 is orally effective in a wide range of human xenograft models, including MV4-11, HT1080, H526, DLD-1, A431, MX-1, MDA-231, MDA-435LM, and glioma 9L. [2] ABT-869 displays antiproliferative and apoptotic effects on cancer cells dependent on mutant kinases, such as FLT3. Consequently, ABT-869 is in clinical studies for the treatment of acute myeloid leukemia (AML). [3, 4] ABT-689 has been shown to induce apoptosis through an AKT and GSK-3beta-dependent pathway, thus suggesting that combination therapies with GSK-3beta inhibitors may be a promising approach to AML treatment. [3]


Technical information:

Chemical Formula:   C21H18FN5O
CAS #:   796967-16-3
Molecular Weight:   375.41
Purity:   > 98%
Appearance:   White
Chemical Name:   1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea
Solubility:   Up to 100 mM in DMSO
Synonyms:   ABT-869, ABT 869, ABT869, AL-39324, AL39324, Linifanib

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Albert et al., Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol. Cancer Ther. 2006, 5, 995-1006. Pubmed ID: 16648571
2. Zhou et al., ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside. J. Hematol. Oncol. 2009, 2, 33-45. Pubmed ID: 19642998
3. Hernandez-Davies et al., The multitargeted receptor tyrosine kinase inhibitor linifanib (ABT-869) induces apoptosis through an Akt and glycogen synthase kinase 3?-dependent pathway. Mol. Cancer Ther. 2011, 10, 949-959. Pubmed ID: 21471285
4. Shankar et al., ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia. Blood, 2007, 109, 3400-3408. Pubmed ID: 19642998

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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