SU-5614

• CAT Number: R055654
• CAS Number: 1055412-47-9
• Molecular Formula: C₁₅H₁₃ClN₂O
• Molecular Weight: 272.73
• Purity: ≥95%
• Target: FLT3
• Solubility: Soluble in DMSO
• Storage: Store at -20C
• InChI: InChI=1S/C15H13ClN2O/c1-8-5-9(2)17-14(8)7-12-11-6-10(16)3-4-13(11)18-15(12)19/h3-7,17H,1-2H3,(H,18,19)/b12-7-
• InChIKey: XLBQNZICMYZIQT-GHXNOFRVSA-N
• SMILES: CC1=CC(=C(N1)C=C2C3=C(C=CC(=C3)Cl)NC2=O)C

SU5614 is a potent and selective FLT3 inhibitor. SU5614 has inhibitory activity for FLT3 and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3. SU5614 reverts the antiapoptotic and pro-proliferative activity of FLT3 ligand (FL) in FL-dependent cells. SU5614 down-regulated the activity of the hyperphosphorylated FLT3 receptor and its downstream targets, signal transducer and activator of (STAT) 3, STAT5, and mitogen-activated protein kinase (MAPK), and the STAT5 target genes BCL-X(L) and p21.

Reference

1: Arseni N, Ahmed F, Hiddemann W, Buske C, Feuring-Buske M. Effects of the protein tyrosine kinase inhibitor, SU5614, on leukemic and normal stem cells. Haematologica. 2005 Nov;90(11):1577-8. PubMed PMID: 16266907.2: Aleskog A, Höglund M, Pettersson J, Hermansson M, Larsson R, Lindhagen E. In vitro activity of the flt3-inhibitor su5614 and standard cytotoxic agents in tumour cells from patients with wild type and mutated flt3 acute myeloid leukaemia. Leuk Res. 2005 Sep;29(9):1079-81. Epub 2005 Apr 15. PubMed PMID: 16038735.3: Spiekermann K, Dirschinger RJ, Schwab R, Bagrintseva K, Faber F, Buske C, Schnittger S, Kelly LM, Gilliland DG, Hiddemann W. The protein tyrosine kinase inhibitor SU5614 inhibits FLT3 and induces growth arrest and apoptosis in AML-derived cell lines expressing a constitutively activated FLT3. Blood. 2003 Feb 15;101(4):1494-504. Epub 2002 Oct 24. PubMed PMID: 12406902.4: Yee KW, O/’Farrell AM, Smolich BD, Cherrington JM, McMahon G, Wait CL, McGreevey LS, Griffith DJ, Heinrich MC. SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase. Blood. 2002 Oct 15;100(8):2941-9. PubMed PMID: 12351406.5: Spiekermann K, Faber F, Voswinckel R, Hiddemann W. The protein tyrosine kinase inhibitor SU5614 inhibits VEGF-induced endothelial cell sprouting and induces growth arrest and apoptosis by inhibition of c-kit in AML cells. Exp Hematol. 2002 Jul;30(7):767-73. PubMed PMID: 12135675.