| 生物活性： |
靶点：c-Kit;c-FMS (CSF-1R)
通路：Angiogenesis; Protein Tyrosine Kinase/RTK
背景说明：Pexidartinib是一种有效的、选择性ATP-竞争性的CSF1R和 c-Kit 抑制剂。Pexidartinib 可以诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。
生物活性：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].
数据来源文献：[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.
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| 其它标识： |
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
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| 基本信息： |
CAS：1029044-16-3
中文名称：培西达替尼
英文名称：Pexidartinib
别名：;Pexidartinib(PLX3397);PLX3397(Pexidartinib);Pexidartinib;
分子式：C20H15ClF3N5
分子量：417.81
规格：10mg ; 5mg
溶解性：Soluble in DMSO(Need ultrasonic)
纯度：≥98%
外观(性状)：Solid
储存条件：Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
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| 靶点： |
c-Kit;c-FMS (CSF-1R) |
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