Pexidartinib (PLX-3397) 是一种有效的,具有口服活性的、选择性ATP-竞争性的集落刺激因子 1(CSF1R 或 M-CSFR)和c-Kit抑制剂,IC50值分别为 20 和 10 nM。Pexidartinib (PLX-3397) 对 c-Kit 和 CSF1R 的选择性是对其他相关激酶的 10-100 倍,例如 FLT3,KDR (VEGFR2),LCK,FLT1 (VEGFR1) 和 NTRK3 (TRKC),IC50值分别为 160,350,860,880 和 890 nM。Pexidartinib (PLX-3397) 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-competitivecolony stimulating factor 1 receptor (CSF1R or M-CSFR)andc-Kitinhibitor, withIC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity forc-Kitand CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cellapoptosisand has anti-tumor activity[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 (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].
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体内研究 (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]. Pexidartinib (50 mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice[4].
Animal Model: | Neonatal mice[2] | Dosage: | 0.25, 1 mg/kg | Administration: | I.P. twice daily for 8 days | Result: | Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells. |
Animal Model: | 10-week old litter mate C57BL/6 mice (chow and high-fat diet fed mice)[4] | Dosage: | 50 mg/kg | Administration: | P.o.; every second day for 3 weeks | Result: | Substantially reduced macrophage numbers in adipose tissue of both chow and high-fat diet fed mice without affecting total myeloid cell levels. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(239.34 mM;Need ultrasonic) 配制储备液 1 mM | 2.3934 mL | 11.9672 mL | 23.9343 mL | 5 mM | 0.4787 mL | 2.3934 mL | 4.7869 mL | 10 mM | 0.2393 mL | 1.1967 mL | 2.3934 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: 5 mg/mL (11.97 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.98 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.98 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.98 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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