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Sunitinib malate

Sunitinib malate

  • CAT Number: I009650
  • CAS Number: 341031-54-7
  • Molecular Formula: C22H27FN4O2
  • Molecular Weight: 398.482
  • Purity: 98%
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Sunitinib (CAT: I009650), also known as SU11248, is the orally bioavailable malate salt of an indolinone-based tyrosine kinase inhibitor with potential antineoplastic activity. Sunitinib was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib blocks the tyrosine kinase activities of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor b (PDGFRb), and c-kit, thereby inhibiting angiogenesis and cell proliferation.

Catalog Number I009650
CAS Number 341031-54-7
Molecular Formula

C22H27FN4O2

Purity 98
Solubility Soluble in DMSO, not in water
Storage 0 - 4°C for short term , or -20°C for long term.
Related CAS 557795-19-4 (free base)
IUPAC Name N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
InChI InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChIKey WINHZLLDWRZWRT-ATVHPVEESA-N
SMILES CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C
Reference

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1:Combination of SL327 and Sunitinib Malate leads to an additive anti-cancer effect in doxorubicin resistant thyroid carcinoma cells. Wang W, Zhou J, Zhao L, Chen S.Biomed Pharmacother. 2017 Apr;88:985-990. doi: 10.1016/j.biopha.2017.01.135. Epub 2017 Feb 6. PMID: 28178630<br />
2:A Novel Positron Emission Tomography (PET) Approach to Monitor Cardiac Metabolic Pathway Remodeling in Response to Sunitinib Malate. O/&#39;Farrell AC, Evans R, Silvola JM, Miller IS, Conroy E, Hector S, Cary M, Murray DW, Jarzabek MA, Maratha A, Alamanou M, Udupi GM, Shiels L, Pallaud C, Saraste A, Liljenb&auml;ck H, Jauhiainen M, Oikonen V, Ducret A, Cutler P, McAuliffe FM, Rousseau JA, Lecomte R, Gascon S, Arany Z, Ky B, Force T, Knuuti J, Gallagher WM, Roivainen A, Byrne AT.PLoS One. 2017 Jan 27;12(1):e0169964. doi: 10.1371/journal.pone.0169964. eCollection 2017. PMID: 28129334 Free PMC Article<br />
3:Targeted drug delivery of Sunitinib Malate to tumor blood vessels by cRGD-chiotosan-gold nanoparticles. Saber MM, Bahrainian S, Dinarvand R, Atyabi F.Int J Pharm. 2017 Jan 30;517(1-2):269-278. doi: 10.1016/j.ijpharm.2016.12.016. Epub 2016 Dec 9. PMID: 27956189<br />
4:In vitro cytotoxic effect of tyrosine kinase inhibitor sunitinib malate alone and in combination with hyperthermia on breast adenocarcinoma MCF-7 cells. Topcul MR, Cetin I.J BUON. 2016 May-Jun;21(3):556-63. PMID: 27569072<br />
5:Oral administration of sunitinib malate for long-term survival of a patient with multiple lung metastases from renal leiomyosarcoma. Li X, Gao H, Tang C, Liu X.Onco Targets Ther. 2016 Jul 29;9:4753-6. doi: 10.2147/OTT.S96473. eCollection 2016. PMID: 27536137 Free PMC Article<br />
6:The tyrosine kinase inhibitor, sunitinib malate, induces cognitive impairment in vivo via dysregulating VEGFR signaling, apoptotic and autophagic machineries. Abdel-Aziz AK, Mantawy EM, Said RS, Helwa R.Exp Neurol. 2016 Sep;283(Pt A):129-41. doi: 10.1016/j.expneurol.2016.06.004. Epub 2016 Jun 7. PMID: 27288242<br />
7:Sunitinib Malate plus Lomustine for Patients with Temozolomide-refractory Recurrent Anaplastic or Low-grade Glioma. Duerinck J, Du Four S, Sander W, Van Binst AM, Everaert H, Michotte A, Hau P, Neyns B.Anticancer Res. 2015 Oct;35(10):5551-7. PMID: 26408725<br />
8:Preclinical Evidence for the Use of Sunitinib Malate in the Treatment of Plexiform Neurofibromas. Ferguson MJ, Rhodes SD, Jiang L, Li X, Yuan J, Yang X, Zhang S, Vakili ST, Territo P, Hutchins G, Yang FC, Ingram DA, Clapp DW, Chen S.Pediatr Blood Cancer. 2016 Feb;63(2):206-13. doi: 10.1002/pbc.25763. Epub 2015 Sep 16. PMID: 26375012 Free PMC Article<br />
9:Sunitinib malate (SU-11248) reduces tumour burden and lung metastasis in an intratibial human xenograft osteosarcoma mouse model. Kumar RM, Arlt MJ, Kuzmanov A, Born W, Fuchs B.Am J Cancer Res. 2015 Jun 15;5(7):2156-68. eCollection 2015. PMID: 26328246 Free PMC Article<br />
10:Effects of sunitinib malate on growth of human bladder transitional cell line T24 in vitro. Wen J, Li HZ, Ji ZG, Jin J.Chin Med Sci J. 2015 Mar;30(1):51-5. PMID: 25837361

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