FI-700

    WARNING: This product is for research use only, not for human or veterinary use.

Description: FI-700 is a novel and potent FLT3 inhibitor with promising antileukemia activity. FI-700 showed a potent IC(50) value against FLT3 kinase at 20 nmol/L in an in vitro kinase assay. FI-700 showed selective growth inhibition against mutant FLT3-expressing leukemia cell lines and primary acute myeloid leukemia cells, whereas it did not affect the FLT3 ligand (FL)-driven growth of Wt-FLT3-expressing cells. Oral administration of FI-700 induced the regression of tumors in a s.c. tumor xenograft model and increased the survival of mice in an i.v. transplanted model. Furthermore, FI-700 treatment eradicated FLT3/ITD-expressing leukemia cells, both in the peripheral blood and in the bone marrow. (Source: Clin Cancer Res. 2007 Aug 1;13(15 Pt 1):4575-82.)

Price and Availability

FI-700 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Synonym: FI700; FI-700; FI 700.

IUPAC/Chemical Name: 5-(5-(piperazin-1-ylmethyl)-1,3,4-oxadiazol-2-yl)-N4-propyl-N2-(2-(pyridin-4-yl)ethyl)pyrimidine-2,4-diamine

InChi Key: AOGSXPPPFJBSRA-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H29N9O/c1-2-6-24-19-17(20-29-28-18(31-20)15-30-12-10-23-11-13-30)14-26-21(27-19)25-9-5-16-3-7-22-8-4-16/h3-4,7-8,14,23H,2,5-6,9-13,15H2,1H3,(H2,24,25,26,27)

SMILES Code: CCCNC1=NC(NCCC2=CC=NC=C2)=NC=C1C3=NN=C(CN4CCNCC4)O3

Technical Data

Additional Information

  
 
 
 

References

1: Kojima K, McQueen T, Chen Y, Jacamo R, Konopleva M, Shinojima N, Shpall E, Huang X, Andreeff M. p53 activation of mesenchymal stromal cells partially abrogates microenvironment-mediated resistance to FLT3 inhibition in AML through HIF-1α-mediated down-regulation of CXCL12. Blood. 2011 Oct 20;118(16):4431-9. doi: 10.1182/blood-2011-02-334136. Epub 2011 Aug 25. PubMed PMID: 21868571; PubMed Central PMCID: PMC3204912.

2: Katsumi A, Kiyoi H, Abe A, Tanizaki R, Iwasaki T, Kobayashi M, Matsushita T, Kaibuchi K, Senga T, Kojima T, Kohno T, Hamaguchi M, Naoe T. FLT3/ ITD regulates leukaemia cell adhesion through α4β1 integrin and Pyk2 signalling. Eur J Haematol. 2011 Mar;86(3):191-8. doi: 10.1111/j.1600-0609.2010.01556.x. Epub 2011 Jan 25. PubMed PMID: 21114537.

3: Kojima K, Konopleva M, Tsao T, Andreeff M, Ishida H, Shiotsu Y, Jin L, Tabe Y, Nakakuma H. Selective FLT3 inhibitor FI-700 neutralizes Mcl-1 and enhances p53-mediated apoptosis in AML cells with activating mutations of FLT3 through Mcl-1/Noxa axis. Leukemia. 2010 Jan;24(1):33-43. doi: 10.1038/leu.2009.212. Epub 2009 Oct 15. PubMed PMID: 19946262.

4: Shiotsu Y. [New therapeutic option for leukemia patients, with FLT3/Aurora kinase inhibitor, KW-2449: strategy and comparison with other kinase inhibitors]. Rinsho Ketsueki. 2008 Aug;49(8):641-9. Review. Japanese. PubMed PMID: 18800614.

5: Stevens AM, Then JE, Frock KM, Crookes BA, Commichau C, Marden BT, Beynnon BJ, Rebuck JA. Evaluation of feeding intolerance in patients with pentobarbital-induced coma. Ann Pharmacother. 2008 Apr;42(4):516-22. doi: 10.1345/aph.1K555. Epub 2008 Mar 25. PubMed PMID: 18364404.

6: Kiyoi H, Shiotsu Y, Ozeki K, Yamaji S, Kosugi H, Umehara H, Shimizu M, Arai H, Ishii K, Akinaga S, Naoe T. A novel FLT3 inhibitor FI-700 selectively suppresses the growth of leukemia cells with FLT3 mutations. Clin Cancer Res. 2007 Aug 1;13(15 Pt 1):4575-82. PubMed PMID: 17671144.