1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. PDGFR
    VEGFR
    Autophagy

Linifanib (Synonyms: ABT-869; AL-39324)

Cat. No.: HY-50751 Purity: 99.42%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
Linifanib Chemical Structure

Linifanib Chemical Structure

CAS No. : 796967-16-3

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10 mM * 1 mL in DMSO $66 In-stock
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Description

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01114191 Abbott Solid Tumors May 2010 Phase 1
NCT00517920 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Hepatocellular Carcinoma September 2007 Phase 2
NCT00517790 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Non-Small Cell Lung Cancer (NSCLC) August 2007 Phase 2
NCT00718380 Abbott Solid Tumor September 2008 Phase 1
NCT00733187 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Solid Tumors February 2009 Phase 1
NCT00486538 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Renal Cell Carcinoma June 2007 Phase 2
NCT00645177 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Metastatic Breast Cancer July 2008 Phase 2
NCT01009593 Abbott Hepatocellular Carcinoma Non-resectable|Hepatocellular Carcinoma Recurrent|Carcinoma, Hepatocellular|Liver Diseases|Neoplasms by Histologic Type|Digestive System Neoplasms|Carcinoma|Liver Neoplasms|Neoplasms|Neoplasms by Site|Digestive System Diseases|Adenocarcinoma|Neoplasms, Glandular and Epithelial January 2010 Phase 3
NCT00754104 Abbott|Genentech, Inc. Solid Tumors September 2008 Phase 1
NCT00716534 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced or Metastatic Non-Small Cell Lung Cancer June 2008 Phase 2
NCT01286974 Abbott Advanced Solid Tumors August 2011 Phase 1
NCT00707889 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Colorectal Cancer|Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum October 2008 Phase 2
NCT00992563 Alcon Research Age Related Macular Degeneration June 2010 Phase 2
NCT01114191 Abbott Solid Tumors May 2010 Phase 1
NCT00517920 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Hepatocellular Carcinoma September 2007 Phase 2
NCT00517790 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Non-Small Cell Lung Cancer (NSCLC) August 2007 Phase 2
NCT00718380 Abbott Solid Tumor September 2008 Phase 1
NCT00733187 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Solid Tumors February 2009 Phase 1
NCT00486538 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Renal Cell Carcinoma June 2007 Phase 2
NCT00645177 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Metastatic Breast Cancer July 2008 Phase 2
NCT01009593 Abbott Hepatocellular Carcinoma Non-resectable|Hepatocellular Carcinoma Recurrent|Carcinoma, Hepatocellular|Liver Diseases|Neoplasms by Histologic Type|Digestive System Neoplasms|Carcinoma|Liver Neoplasms|Neoplasms|Neoplasms by Site|Digestive System Diseases|Adenocarcinoma|Neoplasms, Glandular and Epithelial January 2010 Phase 3
NCT00754104 Abbott|Genentech, Inc. Solid Tumors September 2008 Phase 1
NCT00716534 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced or Metastatic Non-Small Cell Lung Cancer June 2008 Phase 2
NCT01286974 Abbott Advanced Solid Tumors August 2011 Phase 1
NCT00707889 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Advanced Colorectal Cancer|Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum October 2008 Phase 2
NCT00992563 Alcon Research Age Related Macular Degeneration June 2010 Phase 2
NCT01381341 Abbott Advanced Solid Tumors May 2011 Phase 1
NCT01401933 Abbott Advanced Solid Tumors May 2011 Phase 1
NCT01413893 Abbott Advanced Solid Tumors June 2011 Phase 1
NCT01506934 Abbott Advanced or Metastatic Solid Tumors October 2011 Phase 1
NCT01365910 Vanderbilt-Ingram Cancer Center Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer June 2011 Phase 2
NCT01225302 Abbott Non-Small Cell Lung Cancer September 2010 Phase 1
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References
M.Wt

375.4

Formula

C₂₁H₁₈FN₅O

CAS No.

796967-16-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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