| Synonyms: | |
| Status: | Phase 3 |
| Entry Type: | Small molecule |
| Molecule Category: | Parent |
| UNII: | 768FW21J3L |
| InChI Key | GKEYKDOLBLYGRB-LGMDPLHJSA-N |
|---|---|
| Smile | |
| InChI |
|
| Property Name | Value |
|---|---|
| Molecular Formula | C23H27FN4O2 |
| Molecular Weight | 410.49 |
| AlogP | 3.3 |
| Hydrogen Bond Acceptor | 3.0 |
| Hydrogen Bond Donor | 2.0 |
| Number of Rotational Bond | 6.0 |
| Polar Surface Area | 68.44 |
| Molecular species | BASE |
| Aromatic Rings | 2.0 |
| Heavy Atoms | 30.0 |
| Action | Mechanism of Action | Reference |
|---|---|---|
| INHIBITOR | Platelet-derived growth factor receptor inhibitor | DOI PubMed ClinicalTrials |
| Primary Target | |
|---|---|
| kinase insert domain receptor | |
| KIT proto-oncogene, receptor tyrosine kinase | |
| platelet derived growth factor receptor beta |
| Targets | EC50(nM) | IC50(nM) | Kd(nM) | Ki(nM) | Inhibition(%) | |
|---|---|---|---|---|---|---|
|
Enzyme
Kinase
Protein Kinase
TK protein kinase group
Tyrosine protein kinase PDGFR family
|
- | 2 | - | - | - | |
|
Enzyme
Kinase
Protein Kinase
TK protein kinase group
Tyrosine protein kinase VEGFR family
|
- | 2-5 | - | - | - |
| Mesh Heading | Maximum Phase | Mesh ID | Reference |
|---|---|---|---|
| Colorectal Neoplasms | 3 | D015179 | ClinicalTrials |
| Carcinoma, Non-Small-Cell Lung | 3 | D002289 | ClinicalTrials |
| Gastrointestinal Stromal Tumors | 3 | D046152 | ClinicalTrials |
| Carcinoma, Renal Cell | 2 | D002292 | ClinicalTrials |
| Breast Neoplasms | 2 | D001943 | ClinicalTrials |
| Neoplasms | 2 | D009369 | ClinicalTrials |
| Triple Negative Breast Neoplasms | 2 | D064726 | ClinicalTrials |
| Carcinoid Tumor | 2 | D002276 | ClinicalTrials |
| Pancreatic Neoplasms | 2 | D010190 | ClinicalTrials |
| Uterine Cervical Neoplasms | 2 | D002583 | ClinicalTrials |
| Breast Neoplasms | 2 | D001943 | ClinicalTrials |
| Lung Neoplasms | 2 | D008175 | ClinicalTrials |
| Esophageal Neoplasms | 2 | D004938 | ClinicalTrials |
| Cholangiocarcinoma | 2 | D018281 | ClinicalTrials |
| Nasopharyngeal Neoplasms | 2 | D009303 | ClinicalTrials |
| Neoplasms | 2 | D009369 | ClinicalTrials |
| Resources | Reference |
|---|---|
| CAS NUMBER | 1044040-56-3 |
| ChEMBL | CHEMBL1278146 |
| DrugBank | DB11741 |
| FDA SRS | 768FW21J3L |
| Guide to Pharmacology | 7886 |
| PubChem | 16662431 |
| SureChEMBL | SCHEMBL137251 |