1265229-25-1 Usage
Description
Debio-1347, also known as CH5183284, is an orally available and selective inhibitor of fibroblast growth factor receptors (FGFR 1, 2, and 3). It is a promising pharmaceutical candidate with potential applications in various industries due to its ability to target specific receptors and modulate signaling pathways.
Uses
Used in Pharmaceutical Industry:
Debio-1347 is used as a therapeutic agent for the treatment of various cancers. It targets fibroblast growth factor receptors, which play a crucial role in cancer cell proliferation, survival, and angiogenesis. By inhibiting these receptors, Debio-1347 can potentially halt tumor growth and progression.
Debio-1347 is also used as a research tool for studying the role of FGFRs in various biological processes and diseases. It can help researchers understand the underlying mechanisms of FGFR-mediated signaling pathways and identify potential therapeutic targets for the development of novel drugs.
Additionally, Debio-1347 can be used in drug delivery systems to improve the bioavailability and therapeutic outcomes of other anticancer agents. By combining Debio-1347 with other chemotherapeutic drugs, it may enhance their efficacy and overcome drug resistance in cancer treatment.
Biological Activity
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].
Synthesis
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%).
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 1265229-25-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,6,5,2,2 and 9 respectively; the second part has 2 digits, 2 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1265229-25:
(9*1)+(8*2)+(7*6)+(6*5)+(5*2)+(4*2)+(3*9)+(2*2)+(1*5)=151
151 % 10 = 1
So 1265229-25-1 is a valid CAS Registry Number.
1265229-25-1Relevant articles and documents
AMINOPYRAZOLE DERIVATIVE
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, (2012/07/14)
A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C
