Mertk

Mertk产品

所有产品(16)
Mertk抑制剂 (14)
新Mertk产品

目录号	产品名	产品描述	文献引用
S7342	UNC2250	UNC2250是强效的选择性Mer抑制剂，IC50为1.7 nM，比高相关性的酶Axl/Tyro3选择性高了160和60倍。	Bioact Mater, 2024, 32:427-444 Redox Biol, 2022, 54:102366 Front Immunol, 2022, 13:942640
S7638	LDC1267	LDC1267是一种高选择性的TAM kinase抑制剂，对 Mer，Tyro3，和 Axl的IC50分别为<5 nM，8 nM，和 29 nM。对Met，Aurora B，Lck，Src，和 CDK8的活性较低。	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 是一种有效且口服生物可利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM 和 0.8 nM，选择性比作用于Axl和 Tyro3大约高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) 是一种2型ATP竞争型的慢抑制剂，抑制Met (c-Met)酪氨酸激酶，Ki值为2 nM。药效的停留时间为0.00132 min(-1)，t_^1/2为525 min。Merestinib (LY2801653) 还可抑制MST1R、AXL、ROS1、MKNK1/2、FLT3、MERTK、DDR1和DDR2，其对应的IC50值分别为11 nM、2 nM、23 nM、7 nM、7 nM、10 nM、0.1 nM 和 7 nM。	NPJ Breast Cancer, 2024, 10(1):65 Cancers (Basel), 2024, 16(12)2253 J Clin Invest, 2021, 131(11)146987
S9662	UNC2025	UNC2025 是一种有效的、口服活性的 FLT3 和 MER 的双重抑制剂，对应的IC50值分别为0.35 nM和0.46 nM。UNC2025 还抑制 AXL、TRKA、TRKC、QIK、TYRO3、SLK、NuaK1、Kit (c-Kit) 和 Met (c-Met)，对应的IC50值分别为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)是一种可口服的、有效的、选择性的TAM(TYRO3, AXL, MER)/Met (c-Met)抑制剂，在肽段磷酸化实验中具有较低的纳摩尔级别生化活性；在体外激酶结合试验中具有慢速的解离率（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 是一种特异性的Mer tyrosine kinase抑制剂，IC50为 4.3 nM, 其选择性分别超过Axl和Tyro3的选择性 83倍，58倍。	Cell Rep, 2020, 30(11):3671-3681 Front Immunol, 2019, 10:2647
S8404	S49076	S49076是一种新型的、有效的Met (c-Met), AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。	Mol Brain, 2020, 4;13(1):66
S8933	Tamnorzatinib (ONO-7475)	Tamnorzatinib (ONO-7475)是一种有效的、选择性的、口服活性的 Anexelekto(Axl)/MER tyrosine kinase 的新型抑制剂，对于AXL和MER的IC50值分别为0.7 nM和1.0 nM。ONO-7475 在过表达AXL的EGFR突变的NSCLC细胞中可抑制耐受细胞对初始EGFR-TKIs（奥西替尼或达克替尼）的羽化和维持。ONO-7475 可阻滞生长并杀死FMS样酪氨酸激酶3内串联重复突变型急性髓性白血病细胞。	J Cell Mol Med, 2025, 29(1):e70321 Cancer Lett, 2024, 587:216692 Cancer Sci, 2024, 10.1111/cas.16292
G1974^New	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
G1972^New	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 是一种泛 TAM receptor (Axl, Tyro3 and Mertk) 的抑制剂，可阻断Axl受体二聚化位点，对应的Kd值12 μM，IC50值为10 μM。
S6839	MRX-2843	MRX-2843 (UNC2371) 是酪氨酸激酶 MERTK 和 FLT3 的口服活性双重抑制剂，对应的IC50值分别为1.3 nM和0.64 nM。
S0439	UNC2541	UNC2541是一种有效且特异性的Mer酪氨酸激酶(Mer tyrosine kinase, MerTK)抑制剂，可与MerTK ATP口袋结合，IC50为4.4 nM。UNC2541抑制磷酸化的MerTK (pMerTK)，EC50为510 nM。
E1744	UNC5293	UNC5293 是一种有效、高选择性、口服的 MER 受体酪氨酸激酶 (MERTK) 抑制剂，IC50 为 0.9 nM，Ki 为 0.19 nM。
E0142	XL092	XL092 (JUN04542) 是多种 RTK 的 ATP 竞争性抑制剂，包括 MET、VEGFR2、AXL 和 MER，在基于细胞的测定中 IC50 值分别为 15 nM、1.6 nM、3.4 nM 和 7.2 nM。
S7342	UNC2250	UNC2250是强效的选择性Mer抑制剂，IC50为1.7 nM，比高相关性的酶Axl/Tyro3选择性高了160和60倍。	Bioact Mater, 2024, 32:427-444 Redox Biol, 2022, 54:102366 Front Immunol, 2022, 13:942640
S7638	LDC1267	LDC1267是一种高选择性的TAM kinase抑制剂，对 Mer，Tyro3，和 Axl的IC50分别为<5 nM，8 nM，和 29 nM。对Met，Aurora B，Lck，Src，和 CDK8的活性较低。	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 是一种有效且口服生物可利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM 和 0.8 nM，选择性比作用于Axl和 Tyro3大约高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) 是一种2型ATP竞争型的慢抑制剂，抑制Met (c-Met)酪氨酸激酶，Ki值为2 nM。药效的停留时间为0.00132 min(-1)，t_^1/2为525 min。Merestinib (LY2801653) 还可抑制MST1R、AXL、ROS1、MKNK1/2、FLT3、MERTK、DDR1和DDR2，其对应的IC50值分别为11 nM、2 nM、23 nM、7 nM、7 nM、10 nM、0.1 nM 和 7 nM。	NPJ Breast Cancer, 2024, 10(1):65 Cancers (Basel), 2024, 16(12)2253 J Clin Invest, 2021, 131(11)146987
S9662	UNC2025	UNC2025 是一种有效的、口服活性的 FLT3 和 MER 的双重抑制剂，对应的IC50值分别为0.35 nM和0.46 nM。UNC2025 还抑制 AXL、TRKA、TRKC、QIK、TYRO3、SLK、NuaK1、Kit (c-Kit) 和 Met (c-Met)，对应的IC50值分别为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)是一种可口服的、有效的、选择性的TAM(TYRO3, AXL, MER)/Met (c-Met)抑制剂，在肽段磷酸化实验中具有较低的纳摩尔级别生化活性；在体外激酶结合试验中具有慢速的解离率（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 是一种特异性的Mer tyrosine kinase抑制剂，IC50为 4.3 nM, 其选择性分别超过Axl和Tyro3的选择性 83倍，58倍。	Cell Rep, 2020, 30(11):3671-3681 Front Immunol, 2019, 10:2647
S8404	S49076	S49076是一种新型的、有效的Met (c-Met), AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。	Mol Brain, 2020, 4;13(1):66
S8933	Tamnorzatinib (ONO-7475)	Tamnorzatinib (ONO-7475)是一种有效的、选择性的、口服活性的 Anexelekto(Axl)/MER tyrosine kinase 的新型抑制剂，对于AXL和MER的IC50值分别为0.7 nM和1.0 nM。ONO-7475 在过表达AXL的EGFR突变的NSCLC细胞中可抑制耐受细胞对初始EGFR-TKIs（奥西替尼或达克替尼）的羽化和维持。ONO-7475 可阻滞生长并杀死FMS样酪氨酸激酶3内串联重复突变型急性髓性白血病细胞。	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 是一种泛 TAM receptor (Axl, Tyro3 and Mertk) 的抑制剂，可阻断Axl受体二聚化位点，对应的Kd值12 μM，IC50值为10 μM。
S6839	MRX-2843	MRX-2843 (UNC2371) 是酪氨酸激酶 MERTK 和 FLT3 的口服活性双重抑制剂，对应的IC50值分别为1.3 nM和0.64 nM。
S0439	UNC2541	UNC2541是一种有效且特异性的Mer酪氨酸激酶(Mer tyrosine kinase, MerTK)抑制剂，可与MerTK ATP口袋结合，IC50为4.4 nM。UNC2541抑制磷酸化的MerTK (pMerTK)，EC50为510 nM。
E1744	UNC5293	UNC5293 是一种有效、高选择性、口服的 MER 受体酪氨酸激酶 (MERTK) 抑制剂，IC50 为 0.9 nM，Ki 为 0.19 nM。
E0142	XL092	XL092 (JUN04542) 是多种 RTK 的 ATP 竞争性抑制剂，包括 MET、VEGFR2、AXL 和 MER，在基于细胞的测定中 IC50 值分别为 15 nM、1.6 nM、3.4 nM 和 7.2 nM。
G1974^New	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
G1972^New	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