Pexidartinib hydrochloride |
رقم الكتالوجGC34708 |
هيدروكلوريد Pexidartinib (PLX-3397 هيدروكلوريد) هو عامل تحفيز مستعمرة فعال عن طريق الفم وانتقائي ومنافس لـ ATP (CSF1R أو M-CSFR) ومثبط c-Kit ، مع IC50s من 20 و 10 نانومتر ، على التوالييُظهر Pexidartinib هيدروكلوريد انتقائية من 10 إلى 100 ضعف لـ c-Kit و CSF1R على كينازات أخرى ذات صلةيحفز هيدروكلوريد Pexidartinib موت الخلايا المبرمج وله نشاط مضاد للسرطان
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Cas No.: 2040295-03-0
Sample solution is provided at 25 µL, 10mM.
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib exhibits 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]. IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)[1]
Pexidartinib (PLX3397; 0.25, 1 mg/kg, i.p., 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]. Animal Model: Neonatal mice[2]
[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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