Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H21Cl2FN4O3 |
Molecular Weight | 491.342 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=NC=NC(NC3=CC=C(Cl)C(Cl)=C3F)=C2C=C1OC4CCN(CC4)C(=O)C=C
InChI
InChIKey=LPFWVDIFUFFKJU-UHFFFAOYSA-N
InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29)
Molecular Formula | C23H21Cl2FN4O3 |
Molecular Weight | 491.342 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Poziotinib is an inhibitor of EGFR tyrosine kinase family. The drug is being tested in phase II of clinical trials for different cancers: breast cancer, lung adenocarcinoma, head and neck squamous cell carcinoma, HER-2 positive advanced gastric cancer (in combination with Paclitaxel and Trastuzumab).
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2363049 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21732342 |
3.2 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 11.5821 uM] | ||||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | ||||
major | ||||
minor | ||||
minor | ||||
minor | ||||
minor |
Sample Use Guides
Head and Neck Squamous Cell Carcinoma: Take 45 mg orally, daily and continuously. Lung Adenocarcinoma: patients should receive poziotinib at dose of 16 mg orally once daily in a 28-day cycle.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21732342
HCC827 cells were inhibited on 50% at 1.2 nM of poziotinib; NCI-H358 cells - at 4.8 nM; NCI-H1975 cells - at 5.7 nM; Calu-3 cells - at 2.1 nM; NCI-H1781 cells - at 4 nM; SK-Br3 cells - at 1 nM; NCI-N87 cells - at 0.6 nM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:05:19 GMT 2023
by
admin
on
Sat Dec 16 16:05:19 GMT 2023
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Record UNII |
OEI6OOU6IK
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Record Status |
Validated (UNII)
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1742
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NCI_THESAURUS |
C2167
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NCI_THESAURUS |
C129825
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DB12114
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1092364-38-9
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Poziotinib
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CHEMBL3545154
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25127713
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DTXSID80148853
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C98838
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100000177756
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JK-195
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OEI6OOU6IK
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9736
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |