Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H16N8O.H3O4P |
| Molecular Weight | 470.3785 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OP(O)(O)=O.OCCN1C=C(C=N1)C2=CN=C3N=NN(CC4=CC=C5N=CC=CC5=C4)C3=N2
InChI
InChIKey=TWWONGIWZWOGQN-UHFFFAOYSA-N
InChI=1S/C19H16N8O.H3O4P/c28-7-6-26-12-15(9-22-26)17-10-21-18-19(23-17)27(25-24-18)11-13-3-4-16-14(8-13)2-1-5-20-16;1-5(2,3)4/h1-5,8-10,12,28H,6-7,11H2;(H3,1,2,3,4)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19459657 | https://www.ncbi.nlm.nih.gov/pubmed/26013381Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800027901
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19459657 | https://www.ncbi.nlm.nih.gov/pubmed/26013381
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800027901
PF-04217903 is a triazolopyrazine inhibitor of c-MET that displays anticancer chemotherapeutic and anti-metastatic activities. PF-04217903 inhibits cell proliferation, invasion, and migration as well as tumor growth in various cancer models. In animal models of pancreatic neuroendocrine tumors, this compound prevents lymph node metastasis. PF-04217903 had been in phase I clinical trials by Pfizer for the treatment of solid tumors. In 2011, the company discontinued the development of the compound.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.24 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21098644 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PF-04217903 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.81 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21098644 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PF-04217903 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21098644 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PF-04217903 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
16.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21098644 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PF-04217903 plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Sample Use Guides
Escalating doses of PF-04217903 will be administered orally on a continuous dosing schedule. Doses to be evaluated will range from 50 mg BID to 1000 mg BID. A cycle is considered to be 21 days
Route of Administration:
Oral
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NCI_THESAURUS |
C1967
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E1E1K0PK8V
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42623544
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1159490-83-1
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C141443
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ACTIVE MOIETY
SUBSTANCE RECORD
