Molecular structure of ABT-869, CAS Number: 796967-16-3
ABT-869 (CAS 796967-16-3)
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.
QUICK LINKS
Ordering Information
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
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 muM). 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.
ABT-869 (CAS 796967-16-3) References
- Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. | Albert, DH., et al. 2006. Mol Cancer Ther. 5: 995-1006. PMID: 16648571
- ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia. | Shankar, DB., et al. 2007. Blood. 109: 3400-8. PMID: 17209055
- Synergistic antileukemic effects between ABT-869 and chemotherapy involve downregulation of cell cycle-regulated genes and c-Mos-mediated MAPK pathway. | Zhou, J., et al. 2008. Leukemia. 22: 138-46. PMID: 17943175
- ABT-869, a multi-targeted tyrosine kinase inhibitor, in combination with rapamycin is effective for subcutaneous hepatocellular carcinoma xenograft. | Jasinghe, VJ., et al. 2008. J Hepatol. 49: 985-97. PMID: 18930332
- Effect of the multitargeted receptor tyrosine kinase inhibitor, ABT-869 [N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea], on blood pressure in conscious rats and mice: reversal with antihypertensive agents and effect on tumor growth inhibition. | Franklin, PH., et al. 2009. J Pharmacol Exp Ther. 329: 928-37. PMID: 19255283
- ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside. | Zhou, J., et al. 2009. J Hematol Oncol. 2: 33. PMID: 19642998
- Phase I and biomarker study of ABT-869, a multiple receptor tyrosine kinase inhibitor, in patients with refractory solid malignancies. | Wong, CI., et al. 2009. J Clin Oncol. 27: 4718-26. PMID: 19720910
- ABT-869 inhibits the proliferation of Ewing Sarcoma cells and suppresses platelet-derived growth factor receptor beta and c-KIT signaling pathways. | Ikeda, AK., et al. 2010. Mol Cancer Ther. 9: 653-60. PMID: 20197394
- Linifanib (ABT-869) enhances radiosensitivity of head and neck squamous cell carcinoma cells. | Hsu, HW., et al. 2013. Oral Oncol. 49: 591-7. PMID: 23490884
- Linifanib (ABT-869), enhances cytotoxicity with poly (ADP-ribose) polymerase inhibitor, veliparib (ABT-888), in head and neck carcinoma cells. | Hsu, HW., et al. 2014. Oral Oncol. 50: 662-9. PMID: 24735547
- Linifanib (ABT-869) Potentiates the Efficacy of Chemotherapeutic Agents through the Suppression of Receptor Tyrosine Kinase-Mediated AKT/mTOR Signaling Pathways in Gastric Cancer. | Chen, J., et al. 2016. Sci Rep. 6: 29382. PMID: 27387652
- Selection of first-line systemic therapies for advanced hepatocellular carcinoma: A network meta-analysis of randomized controlled trials. | Han, Y., et al. 2021. World J Gastroenterol. 27: 2415-2433. PMID: 34040331
- First-Line Systemic Treatment Strategies for Unresectable Hepatocellular Carcinoma: A Systematic Review and Network Meta-Analysis of Randomized Clinical Trials. | Liu, W., et al. 2021. Front Oncol. 11: 771045. PMID: 35004289
- A Pan-Cancer Analysis Reveals CLEC5A as a Biomarker for Cancer Immunity and Prognosis. | Chen, R., et al. 2022. Front Immunol. 13: 831542. PMID: 35979347
Inhibitor of:
AFP, Ang-2, c-Fms-CSF-1R, c-Kit, Flk-1, Flt-1, Flt-3/Flk-2, Flt-4, MMD, PDGF-A, PDGFR-beta, SCF, Tie-2, TRAF4, and Tyrosine Kinase.Activator of:
Caspase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
ABT-869, 1 mg | sc-359037 | 1 mg | $126.00 | |||
ABT-869, 5 mg | sc-359037A | 5 mg | $582.00 |