Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H26O9P.Na |
Molecular Weight | 452.3679 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 4 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].C[C@@](O)(\C=C\[C@H]1CC=CC(=O)O1)[C@@H](C[C@@H](O)\C=C/C=C\C=C\CO)OP(O)([O-])=O
InChI
InChIKey=XBUIKNRVGYFSHL-IAVQPKKASA-M
InChI=1S/C19H27O9P.Na/c1-19(23,12-11-16-9-7-10-18(22)27-16)17(28-29(24,25)26)14-15(21)8-5-3-2-4-6-13-20;/h2-8,10-12,15-17,20-21,23H,9,13-14H2,1H3,(H2,24,25,26);/q;+1/p-1/b3-2-,6-4+,8-5-,12-11+;/t15-,16+,17+,19+;/m0./s1
Molecular Formula | C19H26O9P |
Molecular Weight | 429.3781 |
Charge | -1 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 4 |
Optical Activity | UNSPECIFIED |
Molecular Formula | Na |
Molecular Weight | 22.9898 |
Charge | 1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P67775 Gene ID: 5515.0 Gene Symbol: PPP2CA Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/9373158 |
3.2 nM [IC50] | ||
Target ID: P60510 Gene ID: 5531.0 Gene Symbol: PPP4C Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/9714542 |
3.0 nM [IC50] | ||
Target ID: P11388|||Q9UQP9 Gene ID: 7153.0 Gene Symbol: TOP2A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/2847752 |
110.0 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.354 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10070885 |
20 mg/m² 1 times / day single, intravenous dose: 20 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
FOSTRIECIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.965 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10070885 |
20 mg/m² 1 times / day single, intravenous dose: 20 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
FOSTRIECIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.76 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10070885 |
20 mg/m² 1 times / day single, intravenous dose: 20 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
FOSTRIECIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
47 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 47 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 47 mg/m2, 1 times / day Sources: Page: p.163 |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: Page: p.163 |
DLT: Fainting, Hypotension... Dose limiting toxicities: Fainting (grade 3, 25%) Sources: Page: p.163Hypotension (grade 1, 25%) Blood creatinine increased (grade 2, 25%) |
20 mg/m2 1 times / day multiple, intravenous Studied dose Dose: 20 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 20 mg/m2, 1 times / day Sources: |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: |
DLT: ALT increased... Disc. AE: Oedema, Hypoalbuminaemia... Dose limiting toxicities: ALT increased (25%) AEs leading todiscontinuation/dose reduction: Oedema (grade 2, 25%) Sources: Hypoalbuminaemia (grade 2, 25%) Proteinuria (25%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hypotension | grade 1, 25% DLT |
47 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 47 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 47 mg/m2, 1 times / day Sources: Page: p.163 |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: Page: p.163 |
Blood creatinine increased | grade 2, 25% DLT |
47 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 47 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 47 mg/m2, 1 times / day Sources: Page: p.163 |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: Page: p.163 |
Fainting | grade 3, 25% DLT |
47 mg/m2 1 times / day multiple, intravenous Highest studied dose Dose: 47 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 47 mg/m2, 1 times / day Sources: Page: p.163 |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: Page: p.163 |
ALT increased | 25% DLT |
20 mg/m2 1 times / day multiple, intravenous Studied dose Dose: 20 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 20 mg/m2, 1 times / day Sources: |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: |
Proteinuria | 25% Disc. AE |
20 mg/m2 1 times / day multiple, intravenous Studied dose Dose: 20 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 20 mg/m2, 1 times / day Sources: |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: |
Hypoalbuminaemia | grade 2, 25% Disc. AE |
20 mg/m2 1 times / day multiple, intravenous Studied dose Dose: 20 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 20 mg/m2, 1 times / day Sources: |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: |
Oedema | grade 2, 25% Disc. AE |
20 mg/m2 1 times / day multiple, intravenous Studied dose Dose: 20 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 20 mg/m2, 1 times / day Sources: |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 4 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Purification of protein phosphatase 4 catalytic subunit: inhibition by the antitumour drug fostriecin and other tumour suppressors and promoters. | 1998 Jul 24 |
|
Stereospecific Formation of E- and Z-Disubstituted Double Bonds by Dehydratase Domains from Modules 1 and 2 of the Fostriecin Polyketide Synthase. | 2017 Oct 11 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10070885
Fostriecin was administered intravenously over 60 min on days 1-5 at 4-week intervals. Dose was escalated from 2 mg m(-2) day(-1) to 20 mg m(-2) day(-1) in 20 patients.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28090813
Fostriecin pretreatment significantly attenuated the inhibitory effects of salbutamol. For that was investigated the effects of fostriecin on the inhibition of histamine release from HLMC, on β-adrenoceptor-driven responses in mast cells and on desensitization. Long-term incubation (24 h) of mast cells with fostriecin (10-6 M) resulted in a significant (p < 0.001) reduction in the maximal response (from 41.2 [± 3.0] to 29.9 [± 4.2] %) to salbutamol following fostriecin treatment.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:49:00 GMT 2023
by
admin
on
Fri Dec 15 15:49:00 GMT 2023
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Record UNII |
8TXS63IX8M
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Record Status |
Validated (UNII)
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Record Version |
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CHEMBL172545
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87860-39-7
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C175067
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |