Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H18N4O |
Molecular Weight | 330.3831 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](NC1=C2C=C(NC2=NC=N1)C3=CC=C(O)C=C3)C4=CC=CC=C4
InChI
InChIKey=XRYJULCDUUATMC-CYBMUJFWSA-N
InChI=1S/C20H18N4O/c1-13(14-5-3-2-4-6-14)23-19-17-11-18(24-20(17)22-12-21-19)15-7-9-16(25)10-8-15/h2-13,25H,1H3,(H2,21,22,23,24)/t13-/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/10850439Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16203782 |
http://en.pharmacodia.com/web/drug/1_14094.html |
https://www.ncbi.nlm.nih.gov/pubmed/23528611
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10850439
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16203782 |
http://en.pharmacodia.com/web/drug/1_14094.html |
https://www.ncbi.nlm.nih.gov/pubmed/23528611
PKI166 is a potent and selective EGFR kinase inhibitor (IC50 = 0.7 nM). PKI166 was tested in phase I clinical trials in patients with advanced solid malignancies, where the recommended dose for further studies was 750 mg once daily for 2 weeks every 4 weeks. In preclinical model, PKI166 was tested in pancreatic, prostate, renal cell, colorectal and other types of cancer. The development of PKI166 was discontinued in 2002 after phase II clinical trials. PKI166 possess antihypertensive properties demonstrated in rat hypertensive chronic kidney disease model.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10850439
Curator's Comment: # Novartis
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P00533|||Q9GZX1 Gene ID: 1956.0 Gene Symbol: EGFR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10850439 |
0.7 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1319 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
750 mg 1 times / day steady-state, oral dose: 750 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2159 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
273 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
403 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
13727 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
750 mg 1 times / day steady-state, oral dose: 750 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
18853 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3334 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3555 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
750 mg 1 times / day steady-state, oral dose: 750 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
16.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
7.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16203782/ |
400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
PKI-166 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
DLT: rash, diarrhea... Other AEs: Fatigue, Anorexia... Dose limiting toxicities: rash (grade 3, 1 pt) Other AEs:diarrhea (grade 3, 1 pt) Alanine aminotransferase increase (grade 3, 1 pt) Fatigue (grades 3-4, 1 pt) Sources: Anorexia (grade 1-2, 2 patients) Nausea (grade 1-2, 4 patients) Vomiting (grade 1-2, 3 patients) Aspartate aminotransferase increase (grade 1-2, 1 pt) |
750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Other AEs: Myalgia, Alanine aminotransferase increase... Other AEs: Myalgia (grade 3-4, 1 pt) Sources: Alanine aminotransferase increase (grade 3-4, 1 pt) abdominal pain (grade 1-2, 3 patients) Fatigue (grade 1-2, 1 pt) Diarrhea (grade 1-2, 11 patient) Rash (grade 1-2, 5 patients) Nausea (grade 1-2, 7 patients) vomiting (grade 1-2, 6 patients) Anorexia (grade 1-2, 1 pt) Aspartate aminotransferase increase (grade 1-2, 4 patients) Dry mouth (grade 1-2, 2 patients) |
100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
DLT: Alanine aminotransferase increase... Other AEs: Nausea, Vomiting... Dose limiting toxicities: Alanine aminotransferase increase (grade 3, 2 patients) Other AEs:Nausea (grade 1-2, 4 patients) Sources: Vomiting (grade 1-2, 3 patients) Anorexia (grade 1-2, 1 pt) Diarrhea (grade 1-2, 2 patients) Rash (grade 1-2, 1 pt) Aspartate aminotransferase increase (grade 1-2, 3 patients) Fatigue (grade 1-2, 3 patients) |
50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
DLT: Alanine aminotransferase increase, Aspartate aminotransferase increase... Other AEs: Abdominal pain, vomiting... Dose limiting toxicities: Alanine aminotransferase increase (grade 3, 1 pt) Other AEs:Aspartate aminotransferase increase (grade 3, 2 patients) Abdominal pain (grade 1-2, 1 pt) Sources: vomiting (grade 1-2, 3 patients) Nausea (grade 1-2, 5 patients) Rash (grade 3-4, 1 pt) Anorexia (grade 1-2, 2 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Aspartate aminotransferase increase | grade 1-2, 1 pt | 900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
Anorexia | grade 1-2, 2 patients | 900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
Vomiting | grade 1-2, 3 patients | 900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
Nausea | grade 1-2, 4 patients | 900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
Alanine aminotransferase increase | grade 3, 1 pt DLT |
900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
diarrhea | grade 3, 1 pt DLT |
900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
rash | grade 3, 1 pt DLT |
900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
Fatigue | grades 3-4, 1 pt | 900 mg 1 times / day multiple, oral (unknown) Highest studied dose Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 5 Sources: |
Anorexia | grade 1-2, 1 pt | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Fatigue | grade 1-2, 1 pt | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Diarrhea | grade 1-2, 11 patient | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Dry mouth | grade 1-2, 2 patients | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
abdominal pain | grade 1-2, 3 patients | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Aspartate aminotransferase increase | grade 1-2, 4 patients | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Rash | grade 1-2, 5 patients | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
vomiting | grade 1-2, 6 patients | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Nausea | grade 1-2, 7 patients | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Alanine aminotransferase increase | grade 3-4, 1 pt | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Myalgia | grade 3-4, 1 pt | 750 mg 1 times / day multiple, oral (unknown) MTD Dose: 750 mg, 1 times / day Route: oral Route: multiple Dose: 750 mg, 1 times / day Sources: |
unhealthy n = 13 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 13 Sources: |
Anorexia | grade 1-2, 1 pt | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Rash | grade 1-2, 1 pt | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Diarrhea | grade 1-2, 2 patients | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Aspartate aminotransferase increase | grade 1-2, 3 patients | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Fatigue | grade 1-2, 3 patients | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Vomiting | grade 1-2, 3 patients | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Nausea | grade 1-2, 4 patients | 100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Alanine aminotransferase increase | grade 3, 2 patients DLT |
100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 8 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 8 Sources: |
Abdominal pain | grade 1-2, 1 pt | 50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
Anorexia | grade 1-2, 2 patients | 50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
vomiting | grade 1-2, 3 patients | 50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
Nausea | grade 1-2, 5 patients | 50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
Alanine aminotransferase increase | grade 3, 1 pt DLT |
50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
Aspartate aminotransferase increase | grade 3, 2 patients DLT |
50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
Rash | grade 3-4, 1 pt | 50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: |
unhealthy n = 7 Health Status: unhealthy Condition: Advanced Solid Malignancies Sex: M+F Food Status: UNKNOWN Population Size: 7 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. | 2000 Jun 1 |
|
Phase I and pharmacologic study of PKI166, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. | 2005 Oct 1 |
|
Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. | 2013 Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16203782
In phase I clinical trials in patients with advanced solid malignancies, PKI166 was first given orally once daily continuously and in the second part of the study once daily for 2 weeks every 4 weeks to establish the maximum tolerated dose. The recommended dose for further studies was 750 mg once daily for 2 weeks every 4 weeks.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10850439
In vitro enzyme assays using EGF-R protein tyrosine kinase was performed in 96-well plates as a filter binding assay. The rate of kinase reaction was measured by a transfer of [γ-33P]ATP to a substrate. PKI166 inhibits EGFR with IC50 of 0.7 nM.
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ACTIVE MOIETY