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產(chǎn)品簡(jiǎn)介 品牌 MedChemExpress (MCE) 貨號(hào) HY-16749 規(guī)格 10 mM * 1 mL;5 mg;10 mg 供貨周期 現(xiàn)貨 應(yīng)用領(lǐng)域 生物產(chǎn)業(yè) Pexidartinib (PLX-3397) 是一種有效、選擇性、ATP-競(jìng)爭(zhēng)性的 CSF1R (cFMS) 和 c-Kit 抑制劑,IC50 值分別為 20 和 10 nM。Pexidartinib 對(duì) c-Kit 和 CSF1R 的選擇性是對(duì)其他相關(guān)激酶的 10-100 倍,例如 FLT3,KDR (VEGFR2),LCK,F(xiàn)LT1 (VEGFR1) 和 NTRK3 (TRKC),IC50
詳細(xì)介紹 "Pexidartinib
產(chǎn)品活性:Pexidartinib (PLX-3397) 是一種有效、選擇性、ATP-競(jìng)爭(zhēng)性的 CSF1R (cFMS) 和 c-Kit 抑制劑,IC50 值分別為 20 和 10 nM。Pexidartinib 對(duì) c-Kit 和 CSF1R 的選擇性是對(duì)其他相關(guān)激酶的 10-100 倍,例如 FLT3,KDR (VEGFR2),LCK,F(xiàn)LT1 (VEGFR1) 和 NTRK3 (TRKC),IC50 值分別為 160,350,860,880 和 890 nM。
研究領(lǐng)域:Protein Tyrosine Kinase/RTK
作用靶點(diǎn):c-Fms | c-Kit
In Vitro: Pexidartinib (PLX3397) 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.
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.Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice.
相關(guān)產(chǎn)品:Drug Repurposing Compound Library | Kinase Inhibitor Library | Clinical Compound Library | Clinical Compound Library Plus | CNS-Penetrant Compound Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library Plus | Bioactive Compound Library Plus | Cabozantinib | Imatinib | BLZ945 | Pazopanib | Sitravatinib | GW2580 | Masitinib | Avapritinib | Dovitinib | SU14813 | Ripretinib | Motesanib | OSI-930 | AST 487 | c-Kit-IN-1 | Amuvatinib | Ki20227 | Edicotinib | Flumatinib | Telatinib | AC710 | AZD2932 | c-Fms-IN-2 | PLX647
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