Debio-1347

Bezeichnung:Debio-1347

CAS-Nr1265229-25-1

Englisch Name:Debio-1347

CBNumberCB12731046

SummenformelC20H16N6O

Molgewicht356.38

MOL-Datei1265229-25-1.mol

Debio-1347 physikalisch-chemischer Eigenschaften

Siedepunkt	775.5±55.0 °C(Predicted)
Dichte	1.51±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	≥35.6 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Aggregatzustand	solid
pka	10.51±0.10(Predicted)
Farbe	Off-white to yellow
CAS Datenbank	1265229-25-1

Debio-1347 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
CH5183284 is an orally available and selective FGFR (fibroblast growth factor receptor) inhibitor acting on FGFR 1, 2, and 3.
Biologische Aktivität
ch5183284 (debio-1347) is a selective and novel inhibitor of fgfr with ic50 value of 9.3, 7.6, 22 and 290 nm for fgfr1, fgfr2, fgfr3 and fgfr4, respectively [1].fibroblast growth factor receptors (fgfrs) are tyrosine kinases and receptors for fibroblast growth factors and consist of fgfr1, fgfr2, fgfr3 and fgfr4. in cancer, fgfr is activated by point mutations, gene amplification or chromosomal translocations/rearrangements and is involved in angiogenesis, cell growth, cell migration, invasion and metastasis [1].ch5183284 (debio-1347) is a selective and novel fgfr inhibitor. in a competitive binding assay, ch5183284 (debio-1347) binding with fgfr1, fgfr2, fgfr3, fgfr4 and kdr with kd values of 20, 20, 25, 740 and 960 nm, respectively. in dms114, snu-16 and kms11 cell lines, ch5183284 (debio-1347) (100-300 nm) inhibited autophosphorylation of fgfr1, fgfr2 and fgfr3. in cancer cell lines with the fgfr genetic alterations, ch5183284 (debio-1347) showed antiproliferative activity [1].in xenograft mouse models, ch5183284 (debio-1347) inhibited tumor growth against xenografts with fgfr genetic alterations such as kg1 (leukemia, fgfr1op-fgfr1 fusion), mfe-280 (endometrial cancer, fgfr2 s252w mutation), snu-16 (gastric cancer, fgfr2 amplification), rt112/84 (bladder cancer, fgfr3-tacc3 fusion) and um-uc-14 (bladder cancer, fgfr3 s249c mutation) by 134%, 100%, 147%, 125% and 116%, respectively [1].
Synthese
The synthesis of Debio-1347 is as follows:
An aqueous solution (1.67 ml) of 4 M sodium hydroxide was added to an ethanol solution (17 ml) of [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1-benzenesulfonyl-1H-indol-2-yl) methanone (87 mg). The resulting mixture was stirred at room temperature for 2 hours. The reaction mixture was poured into water. The resulting solid was collected by filtration, washed with water, and dried to give Debio-1347 (40 mg, 63%).
Einzelnachweise
[1]. nakanishi y, akiyama n, tsukaguchi t, et al. the fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to ch5183284/debio 1347, a novel selective fgfr inhibitor. mol cancer ther, 2014, 13(11): 2547-2558.

Debio-1347 Upstream-Materialien And Downstream Produkte

Debio-1347 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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