ABT-869 (CAS 796967-16-3)

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Alternate Names: Linifanib

Application: ABT-869 is a VEGF (Flk/Flt) and PDGFR inhibitor

CAS Number: 796967-16-3

Molecular Weight: 375.4

Molecular Formula: C₂₁H₁₈FN₅O

Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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SDS & Certificate of Analysis

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ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (Flt/Flk) and PDGFR families (e.g., Flk-1 (KDR), Flt-1, Flt-3/Flk-2, Flt-4, c-Fms-CSF-1R, and c-KIT) demonstrating IC₅₀ values ranging from 4-190 nM. ABT-869 shows little activity against unrelated RTKs, cytoplasmic tyrosine kinases, or Ser/Thr kinases (IC₅₀ > 1 μM). ABT-869 inhibits proliferation in MV-4-11 and MOLM-13 cells (acute myeloid leukemia cell lines harboring RTK mutations; IC₅₀ = 4 and 6 nM, respectively), inducing apoptosis as evidenced by an increased sub-G0/G1 phase cell population, caspase activation, and PARP cleavage. In murine xenograft models, as well as in a phase 1 clinical trial, ABT-869 demonstrated respectable efficacy in solid tumors including lung and hepatocellular carcinomas.

References

1. Albert, D.H. et al. 2006. Mol. Cancer Ther. 5(4): 995-1006. PMID: 16648571
2. Shankar, D.B. et al. 2007. Blood. 109(8): 3400-3408. PMID: 17209055
3. Zhou, J. et al. 2009. J Hematol Oncol. 2 : 33. PMID: 19642998

Physical State :

Solid

Solubility :

Soluble in water (<1 mg/ml at 25° C), DMSO (~20 mg/ml), DMF (~20 mg/ml), 1:5 DMSO:PBS (pH 7.2) (~0.2 mg/ml), ethanol (5 mg/ml at 25° C), and methanol.

Storage :

Store at -20° C

Melting Point :

180-183° C (dec.)

Boiling Point :

542.20° C at 760 mmHg (Predicted)

Density :

1.42 g/cm³ (Predicted)

Refractive Index :

n²⁰_D 1.77 (Predicted)

IC50 :

human endothelial cells: IC₅₀ = 0.2 nM; PDGFR-β: IC₅₀ = 2 nM; KDR: IC₅₀ = 4 nM; CSF-1R: IC₅₀ = 3 nM; Flt1: IC₅₀ = 3 nM; Flt3: IC₅₀ = 4 nM; Vascular endothelial growth factor receptor 2: IC₅₀ = 5 nM (human); Stem cell growth factor receptor: IC₅₀ = 16 nM (human)

pK Values :

pK_a: 13.30 (Predicted), pK_b: 3.67 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

11485656

MDL Number :

MFCD11840918

SMILES :

CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N

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Certificate of Analysis

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ABT-869 (CAS 796967-16-3)

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References

Download SDS (MSDS)

Certificate of Analysis