Flonoltinib maleate
Term · Oncology and biomedicine · MLC-T-ONC-013619
The maleate salt form of flonoltinib, an orally bioavailable dual inhibitor of both Janus-associated kinase 2 (JAK2) and of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon oral administration, flonoltinib targets, binds to and inhibits the activity of both JAK2 and FLT3. This prevents the activation of the JAK/signal transducer and activator of transcription (STAT) signaling pathway and the activation of STAT3 and STAT5 as well as FLT3-mediated signaling. This may lead to an induction of apoptosis and a decrease in proliferation of tumor cells in which JAK2 and FLT3 are overexpressed. In addition, as JAK2 and FLT3 play a key role in the regulation of the inflammatory response and dendritic cell (DC) proliferation, differentiation and function, inhibition of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation of DCs, and may regulate inflammatory and immune responses. JAK2, often upregulated or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key role in tumor cell proliferation and survival. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.
| Identifier | MLC-T-ONC-013619 |
|---|---|
| Field | Oncology and biomedicine |
| Abbreviation | FM |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013619",
"term": "Flonoltinib maleate",
"field": "Oncology and biomedicine",
"definition": "The maleate salt form of flonoltinib, an orally bioavailable dual inhibitor of both Janus-associated kinase 2 (JAK2) and of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon oral administration, flonoltinib targets, binds to and inhibits the activity of both JAK2 and FLT3. This prevents the activation of the JAK/signal transducer and activator of transcription (STAT) signaling pathway and the activation of STAT3 and STAT5 as well as FLT3-mediated signaling. This may lead to an induction of apoptosis and a decrease in proliferation of tumor cells in which JAK2 and FLT3 are overexpressed. In addition, as JAK2 and FLT3 play a key role in the regulation of the inflammatory response and dendritic cell (DC) proliferation, differentiation and function, inhibition of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation of DCs, and may regulate inflammatory and immune responses. JAK2, often upregulated or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key role in tumor cell proliferation and survival. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.",
"abbreviation": "FM",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/flonoltinib-maleate/"
}
Record 7,348 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.