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Identification
NameXL184
Accession NumberDB05153
TypeSmall Molecule
GroupsInvestigational
DescriptionXL184 is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL184 strongly binds to and inhibits several tyrosine receptor kinases. Specifically, XL184 appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression. This agent has also been shown to inhibit mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (Flt3) and tyrosine-protein kinase receptor (Tie-2).
Structure
Thumb
SynonymsNot Available
External IDs Not Available
Product Ingredients Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
CategoriesNot Available
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationInvestigated for use/treatment in solid tumors.
Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of actionXL184 strongly binds to and inhibits several tyrosine receptor kinases. Specifically, XL184 appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression. This agent has also been shown to inhibit mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (Flt3) and tyrosine-protein kinase receptor (Tie-2).
TargetKindPharmacological actionActionsOrganismUniProt ID
Hepatocyte growth factor receptorProteinunknownNot AvailableHumanP08581 details
Vascular endothelial growth factor receptor 2ProteinunknownNot AvailableHumanP35968 details
Mast/stem cell growth factor receptor KitProteinunknownNot AvailableHumanP10721 details
Angiopoietin-1 receptorProteinunknownNot AvailableHumanQ02763 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions Not Available
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External LinksNot Available
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentChildhood Solid Neoplasm / Childhood Thyroid Gland Medullary Carcinoma / Recurrent Childhood Central Nervous System Neoplasm / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Thyroid Gland Carcinoma / Thyroid Gland Medullary Carcinoma1
1Active Not RecruitingTreatmentPancreatic Cancers1
1CompletedTreatmentCancers / Lymphoma NOS / Thyroid Carcinoma1
1CompletedTreatmentCancers / Non-Small-Cell Lung Carcinoma (NSCLC) / Tumors, Solid1
1CompletedTreatmentFollicular Thyroid Cancer / Huerthle Cell Thyroid Cancer / Papillary Thyroid Cancer / Renal Cell Carcinoma (RCC)1
1CompletedTreatmentGiant Cell Glioblastoma / Glioblastomas / Gliosarcoma1
1CompletedTreatmentHealthy Volunteers / Hepatic Impairment1
1CompletedTreatmentHealthy Volunteers / Renal Impairments1
1CompletedTreatmentNeoplasms1
1RecruitingTreatmentAdult Solid Neoplasm / Advanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Human Immunodeficiency Virus (HIV) Infections / Metastatic Malignant Neoplasm / Metastatic Malignant Solid Neoplasm / Recurrent Malignant Neoplasm / Recurrent Malignant Solid Neoplasm / Solid Neoplasms / Unresectable Malignant Neoplasm / Unresectable Solid Neoplasm1
1RecruitingTreatmentClear Cell Renal Cell Carcinoma / Malignant Reproductive System Neoplasm / Malignant Urinary System Neoplasm / Metastatic Urethral Neoplasm / Metastatic Urothelial Carcinoma of the Renal Pelvis and Ureter / Progressive Neoplastic Disease / Recurrent Bladder Carcinoma / Recurrent Urethra Carcinoma / Recurrent Urothelial Carcinoma of the Renal Pelvis and Ureter / Regional Urothelial Carcinoma of the Renal Pelvis and Ureter / Renal Pelvis Urothelial Carcinoma / Solid Neoplasms / Stage III Bladder Adenocarcinoma / Stage III Bladder Squamous Cell Carcinoma / Stage III Bladder Urothelial Carcinoma / Stage III Renal Cell Cancer / Stage III Renal Pelvis Carcinoma / Stage III Ureter Cancer / Stage III Urethral Cancer / Stage IV Bladder Adenocarcinoma / Stage IV Bladder Squamous Cell Carcinoma / Stage IV Bladder Urothelial Carcinoma / Stage IV Renal Cell Cancer / Stage IV Renal Pelvis Carcinoma / Stage IV Ureter Cancer / Stage IV Urethral Cancer / Ureter Urothelial Carcinoma / Urethral Urothelial Carcinoma1
1TerminatedTreatmentRecurrent Melanoma / Stage IIIA Melanoma / Stage IIIB Melanoma / Stage IIIC Melanoma / Stage IV Melanoma / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
1, 2CompletedTreatmentRelapsed Or Refractory Multiple Myeloma1
2Active Not RecruitingDiagnosticBone Metastases / Castrate-resistant Prostate Cancer (CRPC) / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2Active Not RecruitingTreatmentCarcinoid Tumors / Pancreatic Neuroendocrine Tumors (pNET)1
2Active Not RecruitingTreatmentCarcinoma of the Prostate1
2Active Not RecruitingTreatmentClear Cell Renal Cell Carcinoma / Metastatic Renal Cell Cancer / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer1
2Active Not RecruitingTreatmentFallopian Tube Clear Cell Adenocarcinoma / Ovarian Clear Cell Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2Active Not RecruitingTreatmentLung Cancers / Solid Tumor (Not Breast or Prostate Cancers)1
2Active Not RecruitingTreatmentNeurofibromatosis / NF1 / Plexiform Neurofibromas1
2Active Not RecruitingTreatmentNeuroendocrine Carcinoma of the Skin / Skin Cancers1
2Active Not RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC) / Recurrent Non-Small Cell Lung Carcinoma / Stage IV Non-Small Cell Lung Cancer1
2Active Not RecruitingTreatmentRecurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2Active Not RecruitingTreatmentRecurrent Non-Small Cell Lung Carcinoma / Stage IV Non-Small Cell Lung Cancer1
2Active Not RecruitingTreatmentRecurrent Uveal Melanoma / Stage III Uveal Melanoma / Stage IIIA Uveal Melanoma / Stage IIIB Uveal Melanoma / Stage IIIC Uveal Melanoma / Stage IV Uveal Melanoma1
2CompletedTreatmentAstrocytic Tumors1
2CompletedTreatmentCancer, Breast1
2CompletedTreatmentCancers / Tumors, Solid1
2CompletedTreatmentGlioblastoma Multiforme1
2Not Yet RecruitingTreatmentAdrenal Cortex Carcinoma / Adult Alveolar Soft Part Sarcoma / Adult Clear Cell Sarcoma of Soft Parts / Adult Hepatocellular Carcinoma / Adult Rhabdomyosarcoma / Adult Soft Tissue Sarcoma / Childhood Alveolar Soft Part Sarcoma / Childhood Central Nervous System Neoplasm / Childhood Clear Cell Sarcoma of Soft Parts / Childhood Hepatocellular Carcinoma / Childhood Rhabdomyosarcoma / Childhood Soft Tissue Sarcoma / Childhood Solid Neoplasm / Hepatoblastomas / Hepatocellular Carcinomas / Recurrent Adrenal Cortex Carcinoma / Recurrent Adult Hepatocellular Carcinoma / Recurrent Adult Soft Tissue Sarcoma / Recurrent Alveolar Soft Part Sarcoma / Recurrent Childhood Central Nervous System Neoplasm / Recurrent Childhood Hepatocellular Carcinoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma / Recurrent Hepatoblastoma / Recurrent Malignant Solid Neoplasm / Recurrent Renal Cell Carcinoma / Recurrent Rhabdomyosarcoma / Recurrent Solid Neoplasm / Renal Cell Carcinoma (RCC) / Sarcoma, Ewing's / Thyroid Gland Medullary Carcinoma / Wilms Tumor1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentEndometrial Adenosquamous Carcinoma / Endometrial Clear Cell Adenocarcinoma / Endometrial Mixed Adenocarcinoma / Endometrial Serous Adenocarcinoma / Metastatic Endometrioid Adenocarcinoma / Recurrent Uterine Corpus Carcinoma / Stage IV Uterine Corpus Cancer / Stage IVA Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer1
2RecruitingTreatmentNeuroendocrine Tumors1
2RecruitingTreatmentRecurrent Renal Cell Carcinoma / Stage III Renal Cell Cancer / Stage IV Renal Cell Cancer / Type 1 Papillary Renal Cell Carcinoma / Type 2 Papillary Renal Cell Carcinoma1
2SuspendedTreatmentMetastatic Ewing Sarcoma / Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Metastatic Osteosarcoma / Recurrent Ewing Sarcoma / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Osteosarcoma / Stage III Osteosarcoma / Stage IV Osteosarcoma / Stage IVA Osteosarcoma / Stage IVB Osteosarcoma / Unresectable Ewing Sarcoma / Unresectable Osteosarcoma1
2SuspendedTreatmentPoorly Differentiated Thyroid Gland Carcinoma / Recurrent Thyroid Gland Carcinoma / Stage I Thyroid Gland Follicular Carcinoma / Stage I Thyroid Gland Papillary Carcinoma / Stage II Thyroid Gland Follicular Carcinoma / Stage II Thyroid Gland Papillary Carcinoma / Stage III Thyroid Gland Follicular Carcinoma / Stage III Thyroid Gland Papillary Carcinoma / Stage IVA Thyroid Gland Follicular Carcinoma / Stage IVA Thyroid Gland Papillary Carcinoma / Stage IVB Thyroid Gland Follicular Carcinoma / Stage IVB Thyroid Gland Papillary Carcinoma / Stage IVC Thyroid Gland Follicular Carcinoma / Stage IVC Thyroid Gland Papillary Carcinoma / Tall Cell Variant Thyroid Gland Papillary Carcinoma / Thyroid Gland Oncocytic Follicular Carcinoma1
2TerminatedTreatmentCarcinoma of the Prostate / Castration Resistant Prostate Cancer (CRPC) / Prostatic Neoplasms1
2TerminatedTreatmentProstate Cancer Metastatic1
3Active Not RecruitingTreatmentRenal Cell Carcinoma (RCC)1
3Active Not RecruitingTreatmentThyroid Cancers1
3CompletedTreatmentCarcinoma of the Prostate / Castration Resistant Prostate Cancer (CRPC) / Pain / Prostatic Neoplasms1
3RecruitingTreatmentHepatocellular Carcinomas1
4RecruitingTreatmentMedullary Thyroid Cancer (MTC)1
Not AvailableActive Not RecruitingTreatmentAdenocarcinoma of the Prostate / Hormone-Resistant Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
Not AvailableRecruitingDiagnosticAdvanced Cancers / Endocrine Tumors1
Not AvailableRecruitingTreatmentAdenocarcinoma of the Prostate / Castration-Resistant Prostate Cancer (CRPC) / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Predicted ADMET featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to hepatocyte growth factor/HGF ligand. Regulates many physiological processes including proliferation, scattering, morphogenesis and survival. Ligand binding at the cell surface induces autophosphorylation of MET on its intracellular domain that provides docking sites for downstream sig...
Gene Name:
MET
Uniprot ID:
P08581
Molecular Weight:
155540.035 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domai...
Gene Name:
KDR
Uniprot ID:
P35968
Molecular Weight:
151525.555 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1...
Gene Name:
KIT
Uniprot ID:
P10721
Molecular Weight:
109863.655 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Has anti-inflammatory effects by preventing the leakage of proinflammatory plasma proteins and leukocytes from ...
Gene Name:
TEK
Uniprot ID:
Q02763
Molecular Weight:
125829.005 Da
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Drug created on October 21, 2007 16:23 / Updated on August 17, 2016 12:24