Sunitinib malate

Sunitinib malate

Catalog Number:
L002369447APE
Mfr. No.:
APE-A8255
Price:
$188
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      • Overview
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          Background

          Sunitinib malate, also called sunitinib, is a novel, oral, multi-targeted , small molecule oxindole tyrosine kinase inhibitor which inhibits multiple receptor tyrosine kinases including platelet-derived growth factor receptor ( and (, vascular endothelial growth factor receptor 1, 2 and 3, c-KIT, FLT3 kinase, colony-stimulating factor 1 receptor and RET kinase [2][3] [4]. The IC50 of sunitinib is approximately 10-20 ng/ml to NB cell lines, which is within the clinically relevant human trough serum concentration (50-100 ng/ml) [1].
          Receptor tyrosine kinases activated a number of different intracellular signaling pathways [5].
          In neuroblastoma (NB) cell lines, SKN-BE (2), NUB-7, SH-SY5Y and LAN-5, sunitinib significantly inhibited cell proliferation after a treatment for 48 hours, in a concentration-dependent manner [1].
          Treatment with 20, 30 or 40 mg/kg of sunitinib made NOD/SCID mice inoculated with xenograft tumor cells show significant reduction (P

          [1]. Libo Zhang, Kristen M. Smith, Amy Lee Chong, et al. In Vivo Antitumor and Antimetastatic Activity of Sunitinib in Preclinical Neuroblastoma Mouse Model. Neoplasia, 2009, 11: 426-435.
          [2]. Hassane Izzedine, Irina Buhaescu, Olivier Rixe, et al. Sunitinib malate. Cancer Chemother Pharmacol, 2007, 60: 357-364.
          [3]. M. L. Telli, R. M. Witteles, G. A. Fisher, et al. Cardiotoxicity associated with the cancer therapeutic agent sunitinib malate. Annals of Oncology, 2008, 19: 1613–1618.
          [4]. Edwin P. Rock, Vicki Goodman, Janet X. Jiang, et al. Food and Drug Administration Drug Approval Summary: Sunitinib Malate for the Treatment of Gastrointestinal Stromal Tumor and Advanced Renal Cell Carcinoma. The Oncologist, 2007, 12: 107-113.
          [5]. C. J. Marshall. Specificity of Receptor Tyrosine Kinase Signaling: Transient versus Sustained Extracellular Signal-Regulated Kinase Activation. Cel, 1995, 80: 179-185.

      • Properties
        • Alternative Name
          SU 11248,SU11248,SU-11248,Sunitinib; N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide;(2S)-2-hydroxybutanedioic acid
          CAS Number
          341031-54-7
          Molecular Formula
          C22H27FN4O2·C4H6O5
          Molecular Weight
          532.56
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥26.65 mg/mL in DMSO; insoluble in EtOH; ≥4.6 mg/mL in H2O with ultrasonic
          Storage
          Store at 4°C

          * For Research Use Only

      • Reference
        • 1. Wu F, Wu D, et al. "Generation of hepato-biliary organoids from human induced pluripotent stem cells." J Hepatol. 2019 Jan 7. pii: S0168-8278(19)30002-9. PMID:30630011
          2. Lin M, Chen B. "Advances in the drug therapies of acute myeloid leukemia (except acute wpromyelocytic leukemia)." Drug Des Devel Ther. 2018 Apr 30;12:1009-1017. PMID:29750014

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