Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C29H29FN4O |
Molecular Weight | 468.5652 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1
InChI
InChIKey=KPJDVVCDVBFRMU-AREMUKBSSA-N
InChI=1S/C29H29FN4O/c1-35-16-15-31-14-13-20-7-6-8-22(17-20)33-29-32-19-21-18-26(24-10-4-5-12-27(24)30)23-9-2-3-11-25(23)28(21)34-29/h2-12,17,19,26,31H,13-16,18H2,1H3,(H,32,33,34)/t26-/m1/s1
Molecular Formula | C29H29FN4O |
Molecular Weight | 468.5652 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/27627808Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/28161661 | https://www.ncbi.nlm.nih.gov/pubmed/28240679 | https://clinicaltrials.gov/ct2/show/NCT01752920
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/28161661 | https://www.ncbi.nlm.nih.gov/pubmed/28240679 | https://clinicaltrials.gov/ct2/show/NCT01752920
Derazantinib (ARQ 087) is an investigational, oral, multi-kinase inhibitor designed to preferentially inhibit the FGFR family of kinases with demonstrated activity in FGFR2 genetic alterations, including fusions. In human cancers, FGFRs have been found to be dysregulated by multiple mechanisms, including aberrant expression, mutations, chromosomal rearrangements, and amplifications. FGFR dysregulation has been identified as a driver in a number of cancers, including iCCA, cholangiocarcinoma, bladder, endometrial, breast, gastric, lung and ovarian. Current scientific literature suggests FGFR alterations exist in anywhere from 5% to 40% of these cancers. Derazantinib is a potent FGFR inhibitor that shows strong anti-proliferative activity in cell lines harboring FGFR2 alterations. In clinical testing, the molecule has demonstrated activity in cancerous tumors harboring FGFR2 fusions in iCCA and bladder cancers.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4142 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808 |
1.8 nM [IC50] | ||
Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808 |
4.5 nM [IC50] | ||
Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808 |
4.5 nM [IC50] | ||
Target ID: CHEMBL3973 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808 |
34.0 nM [IC50] | ||
Target ID: CHEMBL2041 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808 |
3.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
164.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
DERAZANTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
963.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963 |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DERAZANTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1940.87 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
DERAZANTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
20339.47 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963 |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DERAZANTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5 day EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
DERAZANTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5 day EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28972963 |
300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
DERAZANTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Sample Use Guides
ARQ-087 orally at dose levels specified for their respective dose cohorts on a 28-day schedule. Dosing will begin at 25 mg every other day (QOD) and will escalate until the maximum tolerated dose (MTD)
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27627808
NCI-H716 and SNU-16 cells were plated and incubated at 37°C overnight and subsequently treated with 0.1 μM or 1 μM of ARQ 087 for 24 or 72 hours. The cells were fixed and stained with Cycletest Plus Reagent kit (BD Biosciences, Franklin Lakes, NJ) according to the manufacturer’s instructions, and cell cycle profiles were analyzed using a FACS Calibur flow cytometer
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 20:12:05 GMT 2025
by
admin
on
Mon Mar 31 20:12:05 GMT 2025
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Record UNII |
N9B0H171MJ
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C1967
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NCI_THESAURUS |
C129825
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Code System | Code | Type | Description | ||
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CHEMBL3545421
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PRIMARY | |||
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1814961-15-3
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NO STRUCTURE GIVEN | |||
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C104267
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10488
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46834118
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100000181486
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FG-224
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1234356-69-4
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DB14889
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N9B0H171MJ
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |