| CAS |
1029044-16-3 |
| Chinese Name |
培西达替尼 |
| English Name |
Pexidartinib |
| Synonyms |
;Pexidartinib(PLX3397);PLX3397(Pexidartinib);Pexidartinib; |
| Molecular Formula |
C20H15ClF3N5 |
| Molecular Weight |
417.81 |
| Solubility |
Soluble in DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD28900745 |
| SMILES |
C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F |
| InChIKey |
JGWRKYUXBBNENE-UHFFFAOYSA-N |
| InChI |
InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22，23)24/h1-4，6-8，10-11H，5，9H2，(H，26，27)(H，28，29) |
| PubChem CID |
25151352 |
| Target Point |
c-Kit;c-FMS (CSF-1R) |
| Passage |
Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background |
Pexidartinib is an effective and selective ATP-competitive CSF1R and c-Kit inhibitor. Pexidartinib can induce apoptosis and has anti-tumor activity. |
| Biological Activity |
Pexidartinib (PLX-3397) is a potent， orally active， selective， and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor， with IC50s of 20 and 10 nM， respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity[1]. |
| IC50 |
IC50: 10nM(c-Kit);20nM(cFMS);160nM(FLT3);350nM(KDR);860nM(LCK);880nM(FLT1);890nM(NTRK3)[1] |
| In Vitro |
Pexidartinib(PLX-3397)is a potent，selective and ATP-competitive CSF1R(cFMS)and c-Kit inhibitor，shows 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases，such as FLT3，KDR(VEGFR2)，LCK，FLT1(VEGFR1)and NTRK3(TRKC)，with IC50s of 160，350，860，880，and 890 nM，respectively[1]. |
| In Vivo |
Pexidartinib(PLX3397; 0.25，1 mg/kg，twice daily for 8 days)inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice[2].Pexidartinib(1 mg/kg，twice daily for 8 day)shows no obvious effect on the cleaved caspase-3-positive cells in mice[2]. |
| Data Literature Source |
[1]. DeNardo DG，et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 Jun;1(1):54-67.
[2]. Kuse Y，et al. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018. |
| Unit |
Bottle |
| Specification |
5mg 10mg |
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