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BGJ398 (NVP-BGJ398) - ≥98%, high purity , Fibroblast growth factor receptor inhibitor, CAS No.872511-34-7, Fibroblast growth factor receptor inhibitor

Item Number
N127052
Grouped product items
SKUSizeAvailabilityPrice Qty
N127052-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$48.90
N127052-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$118.90
N127052-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$187.90
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View related series
Apoptosis FGFR fibroblast growth factor receptor 1 Inhibitor fibroblast growth factor receptor 2 Inhibitor fibroblast growth factor receptor 3 Inhibitor fibroblast growth factor receptor 4 Inhibitor kinase insert domain receptor Inhibitor Protein Tyrosine Kinase/RTK

Basic Description

SynonymsBGJ398 (NVP-BGJ398) | 872511-34-7 (free base) | AKOS000295891 | WHO 10032 | 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]-1-methylurea | BCP0726000187 | DB11886 | Infigratinib | Q27075200 | SCHEMBL374435
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological Mechanisms BGJ398 is a potent and selective fibroblast growth factor receptor family inhibitor for Flg (FGFR-1), Bek (FGFR-2), FGFR-3 and FGFR-4.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionFibroblast growth factor receptor inhibitor
Note5mg、25mg卖完停产，不再备货
Product Description

BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor 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. Phase 2.
A potent and selective inhibitor of Flg (FGFR-1), Bek (FGFR-2), FGFR-3 and FGFR-4.

Product Properties

ALogP4.7

Associated Targets(Human)

FGFR1 Tclin Fibroblast growth factor receptor 1 (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGFR2 Tclin Fibroblast growth factor receptor 2 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGFR4 Tclin Fibroblast growth factor receptor 4 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGFR3 Tclin Fibroblast growth factor receptor 3 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SMO Tclin Smoothened homolog (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea
INCHI InChI=1S/C26H31Cl2N7O3/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31)
InChi Key QADPYRIHXKWUSV-UHFFFAOYSA-N
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
Isomeric SMILES CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl
PubChem CID 53235510
Molecular Weight 560.48

Certificates

Certificate of Analysis(COA)

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2 results found

Lot NumberCertificate TypeDateItem
H1814159Certificate of AnalysisFeb 23, 2024 N127052
F1620078Certificate of AnalysisOct 18, 2023 N127052

Chemical and Physical Properties

SolubilityDMSO 1 mg/mL heating (1 mM);Water <1 mg/mL (<1 mM);Ethanol <1 mg/mL (<1 mM)

Related Documents

 SDS

 Specification Sheet

References

1. Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H et al..  (2011)  Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase..  J Med Chem,  54  (20): (7066-83).  [PMID:21936542] [10.1021/op500134e]
2. Komla-Ebri D, Dambroise E, Kramer I, Benoist-Lasselin C, Kaci N, Le Gall C, Martin L, Busca P, Barbault F, Graus-Porta D et al..  (2016)  Tyrosine kinase inhibitor NVP-BGJ398 functionally improves FGFR3-related dwarfism in mouse model..  J Clin Invest,  126  (5): (1871-84).  [PMID:27064282] [10.1021/op500134e]
3. Botrus G, Raman P, Oliver T, Bekaii-Saab T.  (2021)  Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma..  Expert Opin Investig Drugs,  30  (4): (309-316).  [PMID:33307867] [10.1021/op500134e]
4. Lee PC, Hendifar A, Osipov A, Cho M, Li D, Gong J.  (2021)  Targeting the Fibroblast Growth Factor Receptor (FGFR) in Advanced Cholangiocarcinoma: Clinical Trial Progress and Future Considerations..  Cancers (Basel),  13  (7): (1755-70).  [PMID:33916849] [10.3390/cancers13071706]
5. Javle M, Lowery M, Shroff RT, Weiss KH, Springfeld C, Borad MJ, Ramanathan RK, Goyal L, Sadeghi S, Macarulla T et al..  (2018)  Phase II Study of BGJ398 in Patients With FGFR-Altered Advanced Cholangiocarcinoma..  J Clin Oncol,  36  (3): (276-282).  [PMID:29182496] [10.1021/op500134e]

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