Axl

Axl产品

目录号	产品描述	文献引用	实验数据
S1119	Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。	Cancers (Basel), 2021, 13(3)E372 Angiogenesis, 2021, 10.1007/s10456-021-09771-z Nat Commun, 2020, 1;11(1):2124	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S1561	BMS-777607 BMS-777607 (BMS 817378)是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。	J Cell Mol Med, 2021, 10.1111/jcmm.16261 Cell Metab, 2020, 4;31(2):406-421 e7 Cancer Res, 2020, canres.1992.2020	Numbers of clonogenic cells from L3.6pl cells and CSCs＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
S2841	Bemcentinib (R428) Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。	Theranostics, 2021, 11(4):1918-1936 Cancer Res, 2021, canres.1780.2020 EBioMedicine, 2021, 64:103220	Cetuximab-resistant cells are sensitive to therapeutic blockade of AXL activity with the AXL TKI R428. Cells were treated with vehicle (-) or indicated doses of R428 for 24 hours before harvesting whole-cell lysate and immunoblotting for the indicated proteins. α-Tubulin was used as a loading control.
S4001	Cabozantinib malate (XL184) Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， RET (c-RET)， Kit (c-Kit)， Flt-1/3/4， Tie2和AXL，无细胞试验中IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。Cabozantinib malate (XL184)可诱导细胞凋亡。	Sci Adv, 2020, 22;6(21):eaaz8521 Clin Cancer Res, 2020, 20 pii: clincanres Clin Cancer Res, 2020, 8	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S7846	Dubermatinib(TP-0903) TP-0903 是一种有效的选择性 AXL 抑制剂，IC50 为 27 nM。TP-0903 可非常有效地诱导凋亡。	Mol Cell, 2020, 7;S1097-2765(20)30269-0 Cancer Res, 2020, 10.1158/0008-5472.CAN-19-3183 J Exp Clin Cancer Res, 2020, 39(1):197	Phosphorylation of Axl was analyzed by Western blotting of whole cell lysates using different antibodies. GAPDH was used as an internal control. H1299 cells were stimulated for 15 min with 400 nM recombinant human Gas6 (rGas6). H1299 cells were treated with or without TP-0903 (0.2 µmol/L) for 24 h.
S9662New	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。	Front Immunol, 2020, 11:564133
S6870New	Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA)是一种有效的、可口服的 tyrosine kinase，对 c-Met、VEGFR2 和 Axl 的IC50值分别为6.7 nM、1.9 nM和 <1.0 nM。Ningetinib 表现出了抗肿瘤的活性。
S8933New	ONO-7475 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（奥西替尼或达可替尼）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。
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。	Front Immunol, 2020, 11:564133 Nat Commun, 2020, 11(1):3521 Nat Biomed Eng, 2018, 2(8):578-588
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。	Front Microbiol, 2020, 11:1292 Evid Based Complement Alternat Med, 2020, 2020:3205176 Mol Cell, 2019, 10.1016/j.molcel.2019.05.022	Time- and dose-dependent effects of LDC1267 in RSC96 cells.
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
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)，t1/2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。	Front Oncol, 2020, 12;10:700 Cancer Commun (Lond), 2020, 11 J Thorac Oncol, 2019, 14(10):1753-1765
S8570	RXDX-106 (CEP-40783) RXDX-106 (CEP-40783)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）。	J Clin Invest, 2018, 128(11):5034-5055
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。
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
S8573	Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516)是一种新型的、靶向多种参与调节S180肉瘤细胞生长的RTKs的小分子抑制剂，包括c-Kit, PDGFRβ, PDGFRα, c-Met和Axl。	Cancers (Basel), 2020, 12(1)
S8696	2-D08 2-D08 (2',3',4'-trihydroxy flavone) 是一种具有细胞透性的蛋白类泛素化（protein sumoylation）抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。	Cell Res, 2020, 10.1038/s41422-020-00443-z Cell Death Differ, 2020, 10.1038/s41418-020-00641-7
S7754	Gilteritinib (ASP2215) Gilteritinib (ASP2215)是小分子FLT3/AXL抑制剂，对FLT3和AXL的IC50值为0.29 nM和0.73 nM。其抑制c-KIT的IC50值约为抑制FLT3的800倍。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Sci Adv, 2020, 22;6(21):eaaz8521
S7847	SGI-7079 SGI-7079，一种新型选择性Axl抑制剂，体外IC50为58 nM，能以剂量依赖方式抑制肿瘤生长，是克服EFGR抑制剂耐药性的潜在治疗靶标。	Oncotarget, 2017, 8(52):89761-89774	C57BL/6 mice (3 per group) bearing 10-day-established ID8 tumors were treated with control vehicle, R428 or SGI-7079 for 5 days and tumor cells and tumor-infiltrating T cells were analyzed by FACS. (A) The representative FACS plots (left) and statistical results (right) of PD-1 expression on tumor-infiltrating CD4+ T cells and CD8+ T cells.
S7669	NPS-1034 NPS-1034是一种双Met (c-Met)/Axl抑制剂，IC50分别为48 nM和10.3 nM。

目录号	产品描述	文献引用	实验数据
S1119	Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。	Cancers (Basel),2021, 13(3)E372 Angiogenesis,2021, 10.1007/s10456-021-09771-z Nat Commun,2020, 1;11(1):2124	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S1561	BMS-777607 BMS-777607 (BMS 817378)是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。	J Cell Mol Med,2021, 10.1111/jcmm.16261 Cell Metab,2020, 4;31(2):406-421 e7 Cancer Res,2020, canres.1992.2020	Numbers of clonogenic cells from L3.6pl cells and CSCs＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
S2841	Bemcentinib (R428) Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。	Theranostics,2021, 11(4):1918-1936 Cancer Res,2021, canres.1780.2020 EBioMedicine,2021, 64:103220	Cetuximab-resistant cells are sensitive to therapeutic blockade of AXL activity with the AXL TKI R428. Cells were treated with vehicle (-) or indicated doses of R428 for 24 hours before harvesting whole-cell lysate and immunoblotting for the indicated proteins. α-Tubulin was used as a loading control.
S4001	Cabozantinib malate (XL184) Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， RET (c-RET)， Kit (c-Kit)， Flt-1/3/4， Tie2和AXL，无细胞试验中IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。Cabozantinib malate (XL184)可诱导细胞凋亡。	Sci Adv,2020, 22;6(21):eaaz8521 Clin Cancer Res,2020, 20 pii: clincanres Clin Cancer Res,2020, 8	Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
S7846	Dubermatinib(TP-0903) TP-0903 是一种有效的选择性 AXL 抑制剂，IC50 为 27 nM。TP-0903 可非常有效地诱导凋亡。	Mol Cell,2020, 7;S1097-2765(20)30269-0 Cancer Res,2020, 10.1158/0008-5472.CAN-19-3183 J Exp Clin Cancer Res,2020, 39(1):197	Phosphorylation of Axl was analyzed by Western blotting of whole cell lysates using different antibodies. GAPDH was used as an internal control. H1299 cells were stimulated for 15 min with 400 nM recombinant human Gas6 (rGas6). H1299 cells were treated with or without TP-0903 (0.2 µmol/L) for 24 h.
S9662New	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。	Front Immunol,2020, 11:564133
S6870New	Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA)是一种有效的、可口服的 tyrosine kinase，对 c-Met、VEGFR2 和 Axl 的IC50值分别为6.7 nM、1.9 nM和 <1.0 nM。Ningetinib 表现出了抗肿瘤的活性。
S8933New	ONO-7475 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（奥西替尼或达可替尼）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。
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。	Front Immunol,2020, 11:564133 Nat Commun,2020, 11(1):3521 Nat Biomed Eng,2018, 2(8):578-588
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。	Front Microbiol,2020, 11:1292 Evid Based Complement Alternat Med,2020, 2020:3205176 Mol Cell,2019, 10.1016/j.molcel.2019.05.022	Time- and dose-dependent effects of LDC1267 in RSC96 cells.
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
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)，t1/2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。	Front Oncol,2020, 12;10:700 Cancer Commun (Lond),2020, 11 J Thorac Oncol,2019, 14(10):1753-1765
S8570	RXDX-106 (CEP-40783) RXDX-106 (CEP-40783)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）。	J Clin Invest,2018, 128(11):5034-5055
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。
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
S8573	Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516)是一种新型的、靶向多种参与调节S180肉瘤细胞生长的RTKs的小分子抑制剂，包括c-Kit, PDGFRβ, PDGFRα, c-Met和Axl。	Cancers (Basel),2020, 12(1)
S8696	2-D08 2-D08 (2',3',4'-trihydroxy flavone) 是一种具有细胞透性的蛋白类泛素化（protein sumoylation）抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。	Cell Res,2020, 10.1038/s41422-020-00443-z Cell Death Differ,2020, 10.1038/s41418-020-00641-7
S7754	Gilteritinib (ASP2215) Gilteritinib (ASP2215)是小分子FLT3/AXL抑制剂，对FLT3和AXL的IC50值为0.29 nM和0.73 nM。其抑制c-KIT的IC50值约为抑制FLT3的800倍。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Sci Adv,2020, 22;6(21):eaaz8521
S7847	SGI-7079 SGI-7079，一种新型选择性Axl抑制剂，体外IC50为58 nM，能以剂量依赖方式抑制肿瘤生长，是克服EFGR抑制剂耐药性的潜在治疗靶标。	Oncotarget,2017, 8(52):89761-89774	C57BL/6 mice (3 per group) bearing 10-day-established ID8 tumors were treated with control vehicle, R428 or SGI-7079 for 5 days and tumor cells and tumor-infiltrating T cells were analyzed by FACS. (A) The representative FACS plots (left) and statistical results (right) of PD-1 expression on tumor-infiltrating CD4+ T cells and CD8+ T cells.
S7669	NPS-1034 NPS-1034是一种双Met (c-Met)/Axl抑制剂，IC50分别为48 nM和10.3 nM。