Pexidartinib
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Cat.No：IP2270 Solarbio
CAS：1029044-16-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Angiogenesis > Pexidartinib
Product Information
| CAS | 1029044-16-3 |
| Name | 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 |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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