Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C26H31Cl2N7O3 |
| Molecular Weight | 560.475 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCN1CCN(CC1)C2=CC=C(NC3=CC(=NC=N3)N(C)C(=O)NC4=C(Cl)C(OC)=CC(OC)=C4Cl)C=C2
InChI
InChIKey=QADPYRIHXKWUSV-UHFFFAOYSA-N
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)
DescriptionCurator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/ | DOI: 10.1158/2159-8290.CD-NB2014-057 | http://meetinglibrary.asco.org/content/159420-173
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/ | DOI: 10.1158/2159-8290.CD-NB2014-057 | http://meetinglibrary.asco.org/content/159420-173
Infigratinib (BGJ398), a potent, orally bioavailable, small-molecule pan-FGFR kinase inhibitor. FGFR genetic alterations are the most significant predictors for BGJ398 sensitivity. It is currently in phase 2 trials for Cholangiocarcinoma, Glioblastoma and Solid tumors. Detected adverse events were hyperphosphatemia, fatigue, constipation, cough and nausea. Other adverse events were generally mild and included stomatitis, hair loss, decreased appetite, and fatigue.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3650 |
0.9 nM [IC50] | ||
Target ID: CHEMBL4142 |
1.4 nM [IC50] | ||
Target ID: CHEMBL2742 |
1.0 nM [IC50] | ||
Target ID: CHEMBL3973 |
60.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Biophysical characterization of drug-resistant mutants of fibroblast growth factor receptor 1. | 2016 Oct |
|
| Inhibition of FGF Signalling Pathway Augments the Expression of Pluripotency and Trophoblast Lineage Marker Genes in Porcine Parthenogenetic Blastocyst. | 2016 Oct |
|
| Evaluation of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Kinase Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in Fibroblast Growth Factor Receptors: Results of a Global Phase I, Dose-Escalation and Dose-Expansion Study. | 2017 Jan 10 |
Patents
Sample Use Guides
1 x 100 mg and 1 x 25 mg capsules once daily for the first 21 days of the 28-day cycle (3 weeks on, 1 week off in a cycle).
Route of Administration:
Oral
BGJ398 inhibits the proliferation of the FGFR1-, FGFR2-Q, and FGFR3-dependent BaF3 cells with IC50 of 2.9 μM, 2.0 μM and 2 μM, respectively. BGJ398 interferes with autophosphorylation on specific tyrosine residues including FGFR-WT, FGFR2-WT, FGFR3-K650E, FGFR3-S249C and FGFR4-WT with IC50 of 4.6 nM, 4.9 nM, 5 nM, 5 nM and 168 nM, respectively. BGJ398 suppresses proliferation of the cancer cells with wild-type (WT) FGFR3 overexpression such as RT112, RT4, SW780 and JMSU1 with IC50 of 5 nM, 30 nM, 32 nM and 15 nM, respectively.
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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FDA ORPHAN DRUG |
707019
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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NCI_THESAURUS |
C1742
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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NCI_THESAURUS |
C129825
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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FDA ORPHAN DRUG |
833221
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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NCI_THESAURUS |
C1967
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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| Code System | Code | Type | Description | ||
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A4055ME1VK
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CHEMBL1852688
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53235510
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10032
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DB11886
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2550729
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GH-50
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63451
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DTXSID70236238
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admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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Infigratinib
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C88302
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100000172662
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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A4055ME1VK
Created by
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872511-34-7
Created by
admin on Sat Dec 16 07:34:41 UTC 2023 , Edited by admin on Sat Dec 16 07:34:41 UTC 2023
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PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
