WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406207
CAS#: 866883-79-6
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.)
MedKoo Cat#: 406207
Name: FI-700
CAS#: 866883-79-6
Chemical Formula: C21H29N9O
Exact Mass: 423.24951
Molecular Weight: 423.51
Elemental Analysis: C, 59.56; H, 6.90; N, 29.77; O, 3.78
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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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 423.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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.
