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BGJ398

FGFR inhibitor

BGJ398

Catalog No. A3014
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
5mg $80.00 In stock
10mg $120.00 In stock
200mg $780.00 In stock

All inclusive: Shipping and all other fees included

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BGJ398

Related Biological Data

BGJ398
Immunoblot analysis of p-FRS2 and p-ERK1/2 in MRT lines treated with DMSO or NVP-BGJ398 for 40 min as indicated. Total ERK1/2 and b-Tubulin expression was used to monitor equal loading.

Biological Activity

Description BGJ398 (NVP-BGJ398) is a potent and selective inhibitor of FGFR for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
Targets FGFR1 FGFR2 FGFR3 FGFR4    
IC50 0.9 nM 1.4 nM 1 nM 60 nM    

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Chemical Properties

Cas No. 872511-34-7 SDF Download SDF
Synonyms BGJ398,BGJ-398
Chemical Name 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea
Canonical SMILES CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl
Formula C26H31Cl2N7O3 M.Wt 560.48
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

1. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42. doi: 10.1158/1535-7163.MCT-12-0999. Epub 2013 Feb 26.
Abstract
NVP-BGJ398, a selective FGFR inhibitor, is capable of inhibiting FGFR2 signaling, inducing cell-cycle arrest and increasing apoptosis in FGFR2-mutant endometrial cancer cells, which exhibits inhibition against cell growth both in vivo and in vitro.
2. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov. 2012 Dec;2(12):1118-33. doi: 10.1158/2159-8290.CD-12-0210. Epub 2012 Sep 20.
Abstract
Genetic alterations in FGFR family members are potential predictors of NVP-BGJ398 sensitivity, including FGFR1 amplication in osteosarcoma and FGF19 copy number gain at the 11q13 amplicon.

Background

NVP-BGJ398 is a potent, selective, and orally bioavailable inhibitor of the FGFR tyrosine kinases. NVP-BGJ398 is a small molecular with the formula of C26H31Cl2N7O3 and Molecular Weight of 560. The fibroblast growth factor receptor 1 (FGFR1), FGFR2, FGFR3, and FGFR4, encompasses the receptors for 18 different FGF ligands. These ligand–receptor combinations regulate a broad spectrum of signaling during development and in normal growth control. BGJ398 inhibits the cell proliferation and induces apoptosis in cancer cells and suppresses tumor growth in xenograft model.

References:
1. Fibroblast Growth Factor Receptors as Novel Therapeutic Targets in SNF5-Deleted Malignant Rhabdoid Tumors. S Wöhrle, A Weiss, M Ito, A Kauffmann, M Murakami. PLOS ONE. 2013
2. Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth. F Harbinski, VJ Craig, S Sanghavi, D Jeffery, L Liu. Cancer Discovery, 2012