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Signaling Pathway

Linifanib

HY-50751

(ABT-869; AL-39324; ABT 869; ABT869; AL 39324; AL39324)

Linifanib

Linifanib Chemical Structure

Linifanib (ABT-869; AL-39324) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively.

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10 mM * 1 mL in DMSO $66 In-stock
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10 mM * 1 mL in DMSO €65 In-stock
5 mg €59 In-stock
10 mg €98 In-stock
50 mg €343 In-stock
100 mg €588 In-stock
200 mg €1078 In-stock
500 mg €1862 In-stock
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Product name: Linifanib
Cat. No.: HY-50751

Linifanib Data Sheet

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    Purity: 99.8%

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Biological Activity of Linifanib

Linifanib (ABT-869; AL-39324) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively.
IC50 value:  4 nM/3 nM/3 nM/4 nM /66 nM(KDR/CSF-1R/Flt-1/Flt-3PDGFRβ) [1]
Target: VEGFR/PDGFR
in vitro: Linifanib shows inhibitory to Kit, PDGFRβ and Flt4 with IC50 of 14 nM, 66 nM and 190 nM in kinases assay. Linifanib also inhibits ligand-induced KDR, PDGFRβ, Kit, and CSF-1R phosphorylation with IC50 of 2 nM, 2 nM, 31 nM and 10 nM at cellular level and this cellular potency could be affected by serum protein. Linifanib suppresses VEGF-stimulated HUAEC proliferation with IC50 of 0.2 nM. While Linifanib has weak activity against tumor cells which are not induced by VEGF or PDGF, except for MV4-11 leukemia cells (with constitutively active form of Flt3) with IC50 of 4 nM. Linifanib could cause a decrease in S and G2-M phases with a corresponding increase in the sub-G0-G1 apoptotic population in MV4-11 cells [1]. Linifanib binds to the ATP-binding site of CSF-1R with Ki of 3 nM [2]. Linifanib (10 nM) exhibits a reduced phosphorylation of Akt at Ser473 and decreased phosphorylation of GSK3βat Ser9 in Ba/F3 FLT3 ITD cell lines [3].
in vivo: Linifanib (0.3 mg/kg) results in complete inhibition of KDR phosphorylation in lung tissue. Linifanib also inhibits the edema response with ED50 of 0.5 mg/kg. Linifanib (7.5 and 15 mg/kg, bid) significantly inhibits both bFGF- and VEGF-induced angiogenesis in the cornea. Linifanib inhibits tumor growth in flank xenograft models including HT1080, H526, MX-1 and DLD-1 with ED75 from 4.5-12 mg/kg. Linifanib also shows efficacy in A431 and MV4-11 xenografts at low dose levels. Linifanib (12.5 mg/kg bid) reveals a decrease of microvasculure density in MDA-231 xenograft. Linifanib shows a Cmax and AUC24 hours with 0.4 μg/mL and 2.7 μg?hour/mL in HT1080 fibrosarcoma model [1].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 375.4 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C21H18FN5O
CAS No 796967-16-3
Solvent & Solubility

DMSO ≥72mg/mL Water <1.2mg/mL Ethanol ≥4.6mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.6638 mL 13.3191 mL 26.6383 mL
5 mM 0.5328 mL 2.6638 mL 5.3277 mL
10 mM 0.2664 mL 1.3319 mL 2.6638 mL

References on Linifanib

Inhibitor Kit

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