Pexidartinib-hydrochloride-PLX-3397-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPexidartinib hydrochlorideCat. No.: HY-16749ACAS No.: 2040295-03-0Synonyms: PLX-3397 hydrochloride分式: CHClFN分量: 454.28作靶点: c-Fms; c-Kit作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20

2、C 1 month溶解性数据体外实验 DMSO : 60 mg/mL (132.08 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2013 mL 11.0064 mL 22.0129 mL5 mM 0.4403 mL 2.2013 mL 4.4026 mL10 mM 0.2201 mL 1.1006 mL 2.2013 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依

3、次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.50 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.50 mM); Clear solution3. 请依序添加每种溶剂： 10

4、% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.50 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pexidartinib hydrochloride (PLX-3397 hydrochloride)种有效、选择性、ATP-竞争性的 CSF1R (cFMS) 和c-Kit 抑制剂，IC50 值分别为 20 和 10 nM。Pexidartinib 对 c-Kit 和 CSF1R 的选择性是对其他相关激酶的 10-100

5、 倍，例如 FLT3，KDR (VEGFR2)，LCK，FLT1 (VEGFR1) 和 NTRK3 (TRKC)，IC50 值分别为160，350，860，880 和 890 nM。具有抗肿瘤活性 1。IC50 & Target IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM(NTRK3) 1体外研究 Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selecti

6、ve 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.体内研究 Pexidartinib (PLX3397; 0.25, 1 mg

7、/kg, i.p., twice daily for 8 days) inhibits the proliferation of microglia andBrdU-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 cellsin mice 2.Animal Model: Neonatal mice 2Dosage: 0.25, 1 mg/kgAdministration

8、: I.P. twice daily for 8 daysResult: Decreased the number of microglia and BrdU-positive proliferative cells, but did notchange the cleaved caspase-3-positive cells.户使本产品发表的科研献 Neuropharmacology. 2019 Apr 4;151:33-44. Nat Biomed Eng. 2018;2:578-588. Methods Mol Biol. 2018;1711:351-398.See more custo

9、mer validations on HYPERLINK / www.MedChemEREFERENCES1. DeNardo DG, et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. CancerDiscov. 2011 Jun;1(1):54-67.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. 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.McePdfHeightCaution: Product has not been fully validated for