China (Mainland)
Pexidartinib (PLX3397) CAS NO.1029044-16-3
- Min.Order: 0 Metric Ton
- Payment Terms:
- Product Details
Keywords
- Pexidartinib
- PLX3397
- 1029044-16-3
Quick Details
- ProName: Pexidartinib (PLX3397)
- CasNo: 1029044-16-3
- Molecular Formula: C20H15ClF3N5
- ProductionCapacity: Metric Ton/Day
- Purity: >97%
- LimitNum: 0 Metric Ton
Superiority
Biological Activity
| Description | Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3. | ||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
||||||||||||||||||||||||||||||
| In vitro |
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. [1] |
||||||||||||||||||||||||||||||
| Cell Data |
|
||||||||||||||||||||||||||||||
| 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. [1] In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. [2] 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. [3] In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. [4] |