Pexidartinib hydrochloride (PLX-3397 hydrochloride) 是一种有效、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 hydrochloride 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 hydrochloride 可以诱导细胞凋亡 (apoptosis) 具有抗肿瘤活性。
| 生物活性 | Pexidartinib hydrochloride (PLX-3397 hydrochloride) 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 hydrochloride exhibits 10- to 100-fold selectivity forc-Kitand CSF1R over other related kinases. Pexidartinib hydrochloride induces cellapoptosisand has anti-cancer 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 hydrochloride (PLX-3397 hydrochloride) 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].
|
体内研究
(In Vivo) | Pexidartinib hydrochloride (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 hydrochloride (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice[2].
Pexidartinib hydrochloride (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. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 60 mg/mL(132.08 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 | 1 mM | 2.2013 mL | 11.0064 mL | 22.0129 mL | | 5 mM | 0.4403 mL | 2.2013 mL | 4.4026 mL | | 10 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；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 (sealed storage, away from moisture)。-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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 4. 请依序添加每种溶剂： 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution 5. 请依序添加每种溶剂： 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com