product name Pexidartinib (PLX3397)
Description: Pexidartinib, also know as PLX-3397, is an orally available, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease.
References: Cancer Discov. 2011 Jun;1(1):54-67; Mol Med. 2012 May 9;18:519-27; Blood. 2012 Oct 11;120(15):3126-35.
417.81
Formula
C20H15ClF3N5
CAS No.
1029044-16-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 83 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
10% DMSO+40% PEG 300+ddH2O: 15 mg/mL
Synonyms
PLX-3397
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401543
| In Vitro |
In vitro activity: In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. |
| Animal model | MMTV-PyMT mouse model |
| Formulation & Dosage | Formulated in mouse chow; 40 mg/kg; p.o. administration |
| References | Cancer Discov. 2011 Jun;1(1):54-67; Mol Med. 2012 May 9;18:519-27; Blood. 2012 Oct 11;120(15):3126-35. |
Related Posts
product name Pexidartinib (PLX3397)
Description: Pexidartinib, also know as PLX-3397, is an orally available, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease.
References: Cancer Discov. 2011 Jun;1(1):54-67; Mol Med. 2012 May 9;18:519-27; Blood. 2012 Oct 11;120(15):3126-35.
417.81
Formula
C20H15ClF3N5
CAS No.
1029044-16-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 83 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
10% DMSO+40% PEG 300+ddH2O: 15 mg/mL
Synonyms
PLX-3397
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401543
| In Vitro |
In vitro activity: In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. |
| Animal model | MMTV-PyMT mouse model |
| Formulation & Dosage | Formulated in mouse chow; 40 mg/kg; p.o. administration |
| References | Cancer Discov. 2011 Jun;1(1):54-67; Mol Med. 2012 May 9;18:519-27; Blood. 2012 Oct 11;120(15):3126-35. |