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| 商品编号 | 规格 | 价格 | 会员价 | 是否有货 | 数量 |
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| PL04663-5mg | 5mg | ¥964.00 | 请登录 |
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| PL04663-10mg | 10mg | ¥1285.00 | 请登录 |
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| PL04663-50mg | 50mg | ¥3857.00 | 请登录 |
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| PL04663-100mg | 100mg | 询价 | 询价 |
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| PL04663-200mg | 200mg | 询价 | 询价 |
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| PL04663-10mM*1mLinDMSO | 10mM*1mLinDMSO | ¥1060.00 | 请登录 |
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| 中文名称 |
Pexidartinib hydrochloride
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| 英文名称 |
Pexidartinib hydrochloride
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| 英文别名 |
PLX3397 HCl;Pexidartinib hydrochloride;YS6WAI3XN7;Pexidartinib (hydrochloride);Pexidartinib hydrochloride [USAN];Pexidartinib hydrochloride (USAN);5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine hydrochloride;5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine hydrochloride;Turalio (TN);BCP29551
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| Cas No. |
2040295-03-0
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| 分子式 |
C20H16Cl2F3N5
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| 分子量 |
454.28
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| 包装储存 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 产品详情 |
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。
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| 生物活性 |
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC 50 s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)
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| 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 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.
Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice.
Pexidartinib hydrochloride (50?mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| ClinicalTrial |
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| 参考文献 |
[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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| 溶解度数据 |
In Vitro: DMSO : 60 mg/mL (132.08 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic) (insoluble)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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