ABT-869A VEGF (Flk/Flt) and PDGFR inhibitor

ABT-869 (CAS 796967-16-3)

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Application: A VEGF (Flk/Flt) and PDGFR inhibitor
CAS Number: 796967-16-3
Molecular Weight: 375.4
Molecular Formula: C21H18FN5O
* Refer to Certificate of Analysis for lot specific data (including water content).
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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: 995-1006. PMID: 16648571
2. Shankar, D.B., et al. 2007. Blood. 109: 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 :
n20D 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 :
pKa: 13.30 (Predicted), pKb: 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

Download SDS (MSDS)

Certificate of Analysis

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