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PDGFR&FGFR

CH-5183284 (1265229-25-1)

CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

Not Intended for Therapeutic Use. For research use only.

CAS: 1265229-25-1 Category

CH-5183284 (1265229-25-1) Description:

Debio-1347, also known as FF284 and CH5183284, is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity. FGFR inhibitor debio 1347 binds to and inhibits FGFR-1, -2, and -3, which result in the inhibition of FGFR-mediated signal transduction pathways. This leads to the inhibition of both tumor cell proliferation and angiogenesis, and causes cell death in FGFR-overexpressing tumor cells.

In cell-based assay, CH5183284 prevents autophosphorylation of FGFR1, FGFR2, and FGFR3 at 100 to 300 nM in the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 [t(4;14) translocation and FGFR3 Y373C mutation] cell lines. CH5183284 thus produces selective antiproliferative activity against cancer cell lines harboring genetic alterations in FGFR. CH5183284 also inhibit FGFR2 harboring one type of the gatekeeper mutation (V564F) that causes resistance to other FGFR inhibitors.

CH5183284 (100 mg/kg/day, p.o.) shows selective and significant antitumor activity against xenografts with FGFR genetic alterations such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), SNU-16 (gastric cancer, FGFR2 amplification), MFE-280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion).

CH-5183284 (1265229-25-1) Specifications:

Product Name CH-5183284
Synonym Debio-1347; Debio 1347; Debio1347; CH5183284; CH 5183284; CH-5183284; FF284; FF-284; FF 284.
Chemical Name (5-amino-1-(2-methyl-1H-benzo[d]imidazol-6-yl)-1H-pyrazol-4-yl)(1H-indol-2-yl)methanone
Purity ≥98% (HPLC)
CAS Number 1265229-25-1
Molecular Formula C20H16N6O
Molecular Weight 356.389 g/mol
Monoisotopic Mass 356.139 g/mol
MDL number MFCD28502053
InChIKey BEMNJULZEQTDJY-UHFFFAOYSA-N
InChi Code InChI=1S/C20H16N6O/c1-11-23-16-7-6-13(9-17(16)24-11)26-20(21)14(10-22-26)19(27)18-8-12-4-2-3-5-15(12)25-18/h2-10,25H,21H2,1H3,(H,23,24)
SMILES O=C(C1=C(N)N(C2=CC=C3C(NC(C)=N3)=C2)N=C1)C(N4)=CC5=C4C=CC=C5
Form Powder
Color N/A
Solubility  DMSO 71 mg/mL (199.23 mM)

Water Insoluble

Alcohol 3 mg/mL (8.42 mM)

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application selective and orally available FGFR inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Nakanishi Y, et al. Mol Cancer Ther. 2014, 13(11), 2547-2558.

1 review for CH-5183284 (1265229-25-1)

  1. Cofttek

    Never had such good experience before,The CH-5183284 (1265229-25-1) is high purity,also customer service is pretty nice !gotta try!!

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