| Identification | Back Directory | [Name]
1-PHENYL-3-H-8-OXA-2,3-DIAZA-CYCLOPENTA[A]INDEN | [CAS]
34823-86-4 | [Synonyms]
GTP-14564
3-PHENYL-1H-BENZOFURO[3,2-C]PYRAZOLE
1H-Benzofuro[3,2-c]pyrazole, 3-phenyl-
1-PHENYL-3-H-8-OXA-2,3-DIAZA-CYCLOPENTA[A]INDEN | [Molecular Formula]
C15H10N2O | [MDL Number]
MFCD01416326 | [MOL File]
34823-86-4.mol | [Molecular Weight]
234.25 |
| Chemical Properties | Back Directory | [Melting point ]
222-223 °C | [Boiling point ]
459.1±25.0 °C(Predicted) | [density ]
1.321±0.06 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
12.72±0.30(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Description]
GTP 14564 is an inhibitor of class III receptor tyrosine kinases (IC50s = 0.3 μM for c-Fms, c-Kit, ITD-FLT3 and 1 μM for PDGFRβ). It is without effect against a panel of non-receptor tyrosine and serine/threonine kinases. GTP 14564 blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5. | [Uses]
GTP 14564 is a class III receptor tyrosine kinase (RTK) inhibitor. | [Definition]
ChEBI: 3-phenyl-1H-benzofuro[3,2-c]pyrazole is a member of pyrazoles and a ring assembly. | [Biological Activity]
Potent, selective inhibitor of class III receptor tyrosine kinases (IC 50 values are 0.3 μ M for c-Fms, c-Kit, FLT3 and ITD-FLT3 and 1 μ M for PDGFR β ). Displays no selectivity for ERK1, ERK2, EGFR, MEK1, HER2, Src, Abl, PKC, PKA and Akt (IC50 > 10 μ M). Inhibits FL-dependent proliferation in BaF/ITD-FLT3 cells more potently than BaF/wt-FLT3 cells; anti-leukaemic. | [References]
[1] KEN MURATA. Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3).[J]. The Journal of Biological Chemistry, 2003, 278 35: 32892-32898. DOI: 10.1074/jbc.m210405200
[2] Q YAO. Human leukemias with mutated FLT3 kinase are synergistically sensitive to FLT3 and Hsp90 inhibitors: the key role of the STAT5 signal transduction pathway[J]. Leukemia, 2005, 19 9: 1605-1612. DOI: 10.1038/sj.leu.2403881 |
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