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    • Mertk

      Mertk產(chǎn)品

      • 所有產(chǎn)品(16)
      • Mertk抑制劑 (14)
      目錄號(hào) 產(chǎn)品名 產(chǎn)品描述 文獻(xiàn)引用 實(shí)驗(yàn)數(shù)據(jù)
      S7342 UNC2250 UNC2250是強(qiáng)效的選擇性Mer抑制劑,IC50為1.7 nM,比高相關(guān)性的酶Axl/Tyro3選擇性高了160和60倍。
      Bioact Mater, 2024, 32:427-444
      Redox Biol, 2022, 54:102366
      Front Immunol, 2022, 13:942640
      S7638 LDC1267 LDC1267是一種高選擇性的TAM kinase抑制劑,對(duì) Mer,Tyro3,和 Axl的IC50分別為<5 nM,8 nM,和 29 nM。對(duì)Met,Aurora B,Lck,Src,和 CDK8的活性較低。
      Cell Metab, 2021, S1550-4131(21)00326-0
      J Clin Invest, 2021, 131(8)e139434 139434
      J Clin Invest, 2021, 131(8)139434
      S7576 UNC2025 HCl UNC2025 HCl 是一種有效且口服生物可利用的雙重MER/FLT3抑制劑,IC50分別為0.74 nM 和 0.8 nM,選擇性比作用于Axl和 Tyro3大約高20倍。
      Immunity, 2023, 56(8):1778-1793.e10
      Cell Rep, 2022, 38(13):110600
      Cancers (Basel), 2021, 13(23)6072
      S7014 Merestinib (LY2801653) Merestinib (LY2801653) 是一種2型ATP競(jìng)爭(zhēng)型的慢抑制劑,抑制Met (c-Met)酪氨酸激酶,Ki值為2 nM。藥效的停留時(shí)間為0.00132 min(-1),t1/2為525 min。Merestinib (LY2801653) 還可抑制MST1RAXLROS1MKNK1/2FLT3MERTKDDR1DDR2,其對(duì)應(yīng)的IC50值分別為11 nM、2 nM、23 nM、7 nM、7 nM、10 nM、0.1 nM 和 7 nM。
      Mol Oncol, 2025, 19(8):2366-2387
      NPJ Breast Cancer, 2024, 10(1):65
      Cancers (Basel), 2024, 16(12)2253
      S9662 UNC2025 UNC2025 是一種有效的、口服活性的 FLT3MER 的雙重抑制劑,對(duì)應(yīng)的IC50值分別為0.35 nM和0.46 nM。UNC2025 還抑制 AXLTRKATRKCQIKTYRO3SLKNuaK1Kit (c-Kit)Met (c-Met),對(duì)應(yīng)的IC50值分別為1.65 nM、1.67 nM、4.38 nM、5.75 nM、5.83 nM、6.14 nM、7.97 nM、8.18 nM 和 364 nM。
      iScience, 2024, 27(7):110226
      Commun Biol, 2023, 6(1):916
      Commun Biol, 2023, 6(1):916
      S8570 CEP-40783 (RXDX-106) CEP-40783 (RXDX-106)是一種可口服的、有效的、選擇性的TAM(TYRO3, AXL, MER)/Met (c-Met)抑制劑,在肽段磷酸化實(shí)驗(yàn)中具有較低的納摩爾級(jí)別生化活性;在體外激酶結(jié)合試驗(yàn)中具有慢速的解離率(T1/2 >120 min)。
      UNIVERSITY OF CALIFORNIA, 2023,
      bioRxiv, 2023, 2023.10.20.563266
      Mol Cancer Res, 2022, 20(4):542-555
      S7325 UNC2881 UNC2881 是一種特異性的Mer tyrosine kinase抑制劑,IC50為 4.3 nM, 其選擇性分別超過(guò)Axl和Tyro3的選擇性 83倍,58倍。
      Cell Rep, 2020, 30(11):3671-3681
      Front Immunol, 2019, 10:2647
      S8404 S49076 S49076是一種新型的、有效的Met (c-Met), AXL/MERFGFR1/2/3抑制劑,IC50低于20 nM。
      Mol Brain, 2020, 4;13(1):66
      S8933 Tamnorzatinib (ONO-7475) Tamnorzatinib (ONO-7475)是一種有效的、選擇性的、口服活性的 Anexelekto(Axl)/MER tyrosine kinase 的新型抑制劑,對(duì)于AXL和MER的IC50值分別為0.7 nM和1.0 nM。ONO-7475 在過(guò)表達(dá)AXL的EGFR突變的NSCLC細(xì)胞中可抑制耐受細(xì)胞對(duì)初始EGFR-TKIs(奧西替尼或達(dá)克替尼)的羽化和維持。ONO-7475 可阻滯生長(zhǎng)并殺死FMS樣酪氨酸激酶3內(nèi)串聯(lián)重復(fù)突變型急性髓性白血病細(xì)胞。
      J Cell Mol Med, 2025, 29(1):e70321
      Cancer Lett, 2024, 587:216692
      Cancer Sci, 2024, 10.1111/cas.16292
      G1974New AF488 MERTK Antibody [DS5MMER] MerTK is expressed on tissue macrophages and is involved in the removal of apoptotic cells. This process relies on two soluble ligands of MerTK, Protein S and Gas6 that bind to phosphatidylserine found on the outer leaflet of the plasma membrane of cells undergoing apoptosis. Upon binding these ligands, MerTK undergoes autophosphorylation at multiple tyrosine residues that activate the PI3K and Akt pathways. This results in the phagocytosis of apoptotic cells and also results in the direct inhibition of TLR-induced production of pro-inflammatory cytokines. In addition, MerTK may function as a putative entry receptor for filoviruses. Deficiency of MerTK causes general autoimmunity, inflammation and accumulation of apoptotic bodies. MerTK is
      G1972New AF700 MERTK Antibody [DS5MMER] MerTK is expressed on tissue macrophages and is involved in the removal of apoptotic cells. This process relies on two soluble ligands of MerTK, Protein S and Gas6 that bind to phosphatidylserine found on the outer leaflet of the plasma membrane of cells undergoing apoptosis. Upon binding these ligands, MerTK undergoes autophosphorylation at multiple tyrosine residues that activate the PI3K and Akt pathways. This results in the phagocytosis of apoptotic cells and also results in the direct inhibition of TLR-induced production of pro-inflammatory cytokines. In addition, MerTK may function as a putative entry receptor for filoviruses. Deficiency of MerTK causes general autoimmunity, inflammation and accumulation of apoptotic bodies. MerTK is
      S0071 RU-301 RU-301 是一種泛 TAM receptor (Axl, Tyro3 and Mertk) 的抑制劑,可阻斷Axl受體二聚化位點(diǎn),對(duì)應(yīng)的Kd值12 μM,IC50值為10 μM。
      S6839 MRX-2843 MRX-2843 (UNC2371) 是酪氨酸激酶 MERTKFLT3 的口服活性雙重抑制劑,對(duì)應(yīng)的IC50值分別為1.3 nM和0.64 nM。
      S0439 UNC2541 UNC2541是一種有效且特異性的Mer酪氨酸激酶(Mer tyrosine kinase, MerTK)抑制劑,可與MerTK ATP口袋結(jié)合,IC50為4.4 nM。UNC2541抑制磷酸化的MerTK (pMerTK),EC50為510 nM。
      E1744 UNC5293 UNC5293 是一種有效、高選擇性、口服的 MER 受體酪氨酸激酶 (MERTK) 抑制劑,IC50 為 0.9 nM,Ki 為 0.19 nM。
      E0142 XL092 XL092 (JUN04542) 是多種 RTK 的 ATP 競(jìng)爭(zhēng)性抑制劑,包括 MET、VEGFR2、AXL 和 MER,在基于細(xì)胞的測(cè)定中 IC50 值分別為 15 nM、1.6 nM、3.4 nM 和 7.2 nM。
      S7342 UNC2250 UNC2250是強(qiáng)效的選擇性Mer抑制劑,IC50為1.7 nM,比高相關(guān)性的酶Axl/Tyro3選擇性高了160和60倍。
      Bioact Mater, 2024, 32:427-444
      Redox Biol, 2022, 54:102366
      Front Immunol, 2022, 13:942640
      S7638 LDC1267 LDC1267是一種高選擇性的TAM kinase抑制劑,對(duì) Mer,Tyro3,和 Axl的IC50分別為<5 nM,8 nM,和 29 nM。對(duì)Met,Aurora B,Lck,Src,和 CDK8的活性較低。
      Cell Metab, 2021, S1550-4131(21)00326-0
      J Clin Invest, 2021, 131(8)e139434 139434
      J Clin Invest, 2021, 131(8)139434
      S7576 UNC2025 HCl UNC2025 HCl 是一種有效且口服生物可利用的雙重MER/FLT3抑制劑,IC50分別為0.74 nM 和 0.8 nM,選擇性比作用于Axl和 Tyro3大約高20倍。
      Immunity, 2023, 56(8):1778-1793.e10
      Cell Rep, 2022, 38(13):110600
      Cancers (Basel), 2021, 13(23)6072
      S7014 Merestinib (LY2801653) Merestinib (LY2801653) 是一種2型ATP競(jìng)爭(zhēng)型的慢抑制劑,抑制Met (c-Met)酪氨酸激酶,Ki值為2 nM。藥效的停留時(shí)間為0.00132 min(-1),t1/2為525 min。Merestinib (LY2801653) 還可抑制MST1RAXLROS1MKNK1/2FLT3MERTKDDR1DDR2,其對(duì)應(yīng)的IC50值分別為11 nM、2 nM、23 nM、7 nM、7 nM、10 nM、0.1 nM 和 7 nM。
      Mol Oncol, 2025, 19(8):2366-2387
      NPJ Breast Cancer, 2024, 10(1):65
      Cancers (Basel), 2024, 16(12)2253
      S9662 UNC2025 UNC2025 是一種有效的、口服活性的 FLT3MER 的雙重抑制劑,對(duì)應(yīng)的IC50值分別為0.35 nM和0.46 nM。UNC2025 還抑制 AXLTRKATRKCQIKTYRO3SLKNuaK1Kit (c-Kit)Met (c-Met),對(duì)應(yīng)的IC50值分別為1.65 nM、1.67 nM、4.38 nM、5.75 nM、5.83 nM、6.14 nM、7.97 nM、8.18 nM 和 364 nM。
      iScience, 2024, 27(7):110226
      Commun Biol, 2023, 6(1):916
      Commun Biol, 2023, 6(1):916
      S8570 CEP-40783 (RXDX-106) CEP-40783 (RXDX-106)是一種可口服的、有效的、選擇性的TAM(TYRO3, AXL, MER)/Met (c-Met)抑制劑,在肽段磷酸化實(shí)驗(yàn)中具有較低的納摩爾級(jí)別生化活性;在體外激酶結(jié)合試驗(yàn)中具有慢速的解離率(T1/2 >120 min)。
      UNIVERSITY OF CALIFORNIA, 2023,
      bioRxiv, 2023, 2023.10.20.563266
      Mol Cancer Res, 2022, 20(4):542-555
      S7325 UNC2881 UNC2881 是一種特異性的Mer tyrosine kinase抑制劑,IC50為 4.3 nM, 其選擇性分別超過(guò)Axl和Tyro3的選擇性 83倍,58倍。
      Cell Rep, 2020, 30(11):3671-3681
      Front Immunol, 2019, 10:2647
      S8404 S49076 S49076是一種新型的、有效的Met (c-Met), AXL/MERFGFR1/2/3抑制劑,IC50低于20 nM。
      Mol Brain, 2020, 4;13(1):66
      S8933 Tamnorzatinib (ONO-7475) Tamnorzatinib (ONO-7475)是一種有效的、選擇性的、口服活性的 Anexelekto(Axl)/MER tyrosine kinase 的新型抑制劑,對(duì)于AXL和MER的IC50值分別為0.7 nM和1.0 nM。ONO-7475 在過(guò)表達(dá)AXL的EGFR突變的NSCLC細(xì)胞中可抑制耐受細(xì)胞對(duì)初始EGFR-TKIs(奧西替尼或達(dá)克替尼)的羽化和維持。ONO-7475 可阻滯生長(zhǎng)并殺死FMS樣酪氨酸激酶3內(nèi)串聯(lián)重復(fù)突變型急性髓性白血病細(xì)胞。
      J Cell Mol Med, 2025, 29(1):e70321
      Cancer Lett, 2024, 587:216692
      Cancer Sci, 2024, 10.1111/cas.16292
      S0071 RU-301 RU-301 是一種泛 TAM receptor (Axl, Tyro3 and Mertk) 的抑制劑,可阻斷Axl受體二聚化位點(diǎn),對(duì)應(yīng)的Kd值12 μM,IC50值為10 μM。
      S6839 MRX-2843 MRX-2843 (UNC2371) 是酪氨酸激酶 MERTKFLT3 的口服活性雙重抑制劑,對(duì)應(yīng)的IC50值分別為1.3 nM和0.64 nM。
      S0439 UNC2541 UNC2541是一種有效且特異性的Mer酪氨酸激酶(Mer tyrosine kinase, MerTK)抑制劑,可與MerTK ATP口袋結(jié)合,IC50為4.4 nM。UNC2541抑制磷酸化的MerTK (pMerTK),EC50為510 nM。
      E1744 UNC5293 UNC5293 是一種有效、高選擇性、口服的 MER 受體酪氨酸激酶 (MERTK) 抑制劑,IC50 為 0.9 nM,Ki 為 0.19 nM。
      E0142 XL092 XL092 (JUN04542) 是多種 RTK 的 ATP 競(jìng)爭(zhēng)性抑制劑,包括 MET、VEGFR2、AXL 和 MER,在基于細(xì)胞的測(cè)定中 IC50 值分別為 15 nM、1.6 nM、3.4 nM 和 7.2 nM。
      G1974New AF488 MERTK Antibody [DS5MMER] MerTK is expressed on tissue macrophages and is involved in the removal of apoptotic cells. This process relies on two soluble ligands of MerTK, Protein S and Gas6 that bind to phosphatidylserine found on the outer leaflet of the plasma membrane of cells undergoing apoptosis. Upon binding these ligands, MerTK undergoes autophosphorylation at multiple tyrosine residues that activate the PI3K and Akt pathways. This results in the phagocytosis of apoptotic cells and also results in the direct inhibition of TLR-induced production of pro-inflammatory cytokines. In addition, MerTK may function as a putative entry receptor for filoviruses. Deficiency of MerTK causes general autoimmunity, inflammation and accumulation of apoptotic bodies. MerTK is
      G1972New AF700 MERTK Antibody [DS5MMER] MerTK is expressed on tissue macrophages and is involved in the removal of apoptotic cells. This process relies on two soluble ligands of MerTK, Protein S and Gas6 that bind to phosphatidylserine found on the outer leaflet of the plasma membrane of cells undergoing apoptosis. Upon binding these ligands, MerTK undergoes autophosphorylation at multiple tyrosine residues that activate the PI3K and Akt pathways. This results in the phagocytosis of apoptotic cells and also results in the direct inhibition of TLR-induced production of pro-inflammatory cytokines. In addition, MerTK may function as a putative entry receptor for filoviruses. Deficiency of MerTK causes general autoimmunity, inflammation and accumulation of apoptotic bodies. MerTK is
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