CSF-1R

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研究领域

抑制剂选择性比较

CSF-1R产品

所有产品(18) CSF-1R抑制剂(18)

目录号	产品描述	文献引用	实验数据
S1035	Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。	NPJ Breast Cancer, 2022, 8(1):44 Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancer Cell, 2021, S1535-6108(21)00659-0	Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S1003	Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635)是一种新型有效的ATP竞争性VEGFR/PDGFR抑制剂，作用于KDR，CSF-1R，Flt-1/3和PDGFRβ，其IC50分别为4 nM，3 nM，3 nM/4 nM和66 nM，对突变激酶依赖性癌细胞（即FLT3）最有效。Linifanib (ABT-869) 可诱导自噬和凋亡。Phase 3。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cell Rep Med, 2022, 3(1):100492 Cancer Lett, 2021, 507:80-88	(B and C) KMCH-1 cells were plated alone (monoculture) or together with PDGF-BB-secreting LX-2 cells (co-culture) in a transwell insert co-culture system (KMCH-1 cells in the bottom wells and LX-2 cells in the inserts; 1:1 ratio) for 2 days. Cells were treated as indicated with vehicle, rhTRAIL (10 ng/ml for 6 h on day 2), rhTRAIL plus imatinib [rhTRAIL:10 ng/ml for 6 h on day 2; Imatinib: 5 μmol/L for 24 h (day2)], or rhTRAIL plus linifanib [rhTRAIL: 10 ng/ml for 6 h on day 2; Linifanib:0.5 μmol/L for 24 h (day2)]. After rhTRAIL treatment for 6 h,KMCH-1 cells were analysed for apoptotic nuclear morphology by DAPI-staining (B) and for DNA fragmentation by transferasemediated dUTP nick end labelling assay (C) with quantification of apoptotic nuclei by fluorescence microscopy.
S1181	ENMD-2076 ENMD-2076 选择性地作用于 Aurora A 和 Flt3，IC50分别为14 nM和1.86 nM，作用于Aurora A比作用于Aurora B选择性高25倍，对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα作用效果稍弱。ENMD-2076 可抑制各种人类实体瘤和造血癌细胞系的生长，其IC50值为0.025至0.7μM，可诱导凋亡和G2/M期停滞。Phase 2。	Cell, 2021, 184(2):334-351.e20 Sci Adv, 2021, 7(4)eabd7851 J Pediatr Hematol Oncol, 2019, 41(6):e359-e370	Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
S1189	Aprepitant (MK-0869) Aprepitant (MK-0869, L-754030)是一种有效的选择性 neurokinin-1 receptor 拮抗剂，IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平，包括 G-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。	Cancers (Basel), 2021, 13(15)3871 Phytomedicine, 2021, 95:153864 Nat Commun, 2020, 29;11(1):2673	HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.
S1220	OSI-930 OSI-930是一种有效的Kit (c-Kit)， KDR和CSF-1R抑制剂，IC50分别为80 nM， 9 nM和15 nM，对Flt-1， c-Raf和Lck具有适度的抑制活性，对PDGFRα/β， Flt-3和Abl抑制活性较弱。Phase 1。	Cell Rep, 2019, 28(9):2331-2344 Nat Biomed Eng, 2018, 2(8):578-588 Mol Syst Biol, 2015, 11(1):789	RE-luc2P-HEK293 cells were pretreated with 1uM OSI-930 (green), 20uM TBB (blue), 10uM CKI-7 (purple), or 10uM H-89 (orange) for 16 h and infected with Y. enterocolitica WA or Y. pestis Ind195 at MOI 1 and 20, respectively, for 1 h. Following stimulation with 10 ng/ml TNF-α at 5 h post-infection, luciferase activity was measured 24 h post-infection. Results were determined from two independent experiments performed in triplicate. A"*" denotes that the % NF-κβ inhibition using the inhibitors was significantly different (p<0.05) compared to the no drug control (black). The relative NF-κB inhibition by Yersinia infection was determined as a percentage of luciferase activity in bacteria-infected cells relative to luciferase activity in bacteria-free control cells.
S9620^New	Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) 是一种有效的 MET/CSF1R/SRC 抑制剂，IC50 分别为 0.14 nM、0.71 nM 和 0.12 nM。TPX-0022 在临床前模型中可调节肿瘤免疫微环境。
S3012	Pazopanib Pazopanib (GW786034) 是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms/CSF1R抑制剂，无细胞试验中IC50分别为10 nM，30 nM，47 nM，84 nM，74 nM，140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。	NPJ Breast Cancer, 2022, 8(1):44 J Pharmacol Exp Ther, 2022, 380(2):114-125 Birth Defects Res, 2022, 10.1002/bdr2.2001	Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S8042	GW2580 GW2580 (SC-203877) 是一种选择性CSF-1R抑制剂，作用于c-FMS时，IC50为30 nM，比作用于b-Raf， CDK4， c-KIT， c-SRC， EGFR， ERBB2/4， ERK2， FLT-3， GSK3， ITK， JAK2等的选择性高150到500倍。	Brain Behav Immun, 2021, S0889-1591(21)00097-0 Cardiovasc Res, 2020, 10.1093/cvr/cvaa046 Neurobiol Dis, 2020, 134:104705	CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, GW2580 (C) for 8 days. Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay.
S8015	Agerafenib (RXDX-105) Agerafenib (RXDX-105, CEP-32496) 是一种高度有效的BRAF(V600E/WT)和c-Raf抑制剂，K_d为14 nM/36 nM和39 nM，适度有效作用于Abl-1， c-Kit， RET (c-RET)， PDGFRβ和VEGFR2，对MEK-1， MEK-2， ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。	Mol Pharmacol, 2021, 99(6):435-447 Dis Model Mech, 2020, dmm.047779 Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520
S8721	PDGFR inhibitor 1 PDGFR inhibitor 1是一种具有口服活性的Kit (c-Kit)和PDGFR抑制剂，具有潜在的抗肿瘤活性。它还能抑制好几种其他激酶，包括VEGFR2、TIE2、PDGFR-beta和CSF1R，因此进而抑制肿瘤细胞的生长。	Oncogene, 2022, 41(20):2860-2872
S7688	Ki20227 Ki20227 是一种口服活性的 c-Fms tyrosine kinase(CSF1R) 的高选择性抑制剂，对 c-Fms、vascular endothelial growth factor receptor-2 (KDR/VEGFR-2)、stem cell factor receptor (c-Kit) 和 platelet-derived growth factor receptor beta (PDGFRβ) 的IC50值为2 nM、12 nM、451 nM和217 nM。
S8401	Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂，具有潜在的抗肿瘤活性。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。	JCI Insight, 2022, 7(7)e154824 Oncoimmunology, 2022, 11(1):2021619 Hum Cell, 2022, 10.1007/s13577-022-00671-y	E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493
S3570	ARRY-382 ARRY-382 是 CSF1R 的高选择性口服抑制剂，IC50 为 9 nM。
S8578	PRN1371 PRN1371是FGFR1-4的不可逆性共价抑制剂，对于FGFR1, 2, 3, 4和CSF1R的IC50分别为0.6、1.3、4.1、19.3、和8.1 nM。	Nat Commun, 2021, 12(1):6572
S7725	BLZ945 BLZ945是一种具有口服活性的，有效的选择性 CSF-1R抑制剂，IC50为1 nM，比其最接近的受体酪氨酸激酶同系物高出1000多倍的选择性。	Proc Natl Acad Sci U S A, 2022, 119(14):e2111804119 Cell Death Dis, 2022, 13(2):166 Nat Commun, 2021, 12(1):1858	CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, BLZ945 (B) for 8 days Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay.
S7818	Pexidartinib (PLX3397) Pexidartinib (PLX3397)是一种口服有效的多靶点CSF-1R，Kit (c-Kit)，和 FLT3受体酪氨酸激酶抑制剂，其IC50分别为20 nM, 10 nM 和 160 nM。Pexidartinib (PLX3397) 可以诱导细胞凋亡和坏死，并具有抗肿瘤活性。Phase 3。	J Clin Invest, 2022, 132(3)e145071 Aging Cell, 2022, 10.1111/acel.13623 Int J Mol Sci, 2022, 23(5)2793	(a) Reduced tumour burden in PLX3397 (PLX) treated mice relative to untreated (NT) (n=6, P=.015; unpaired t-test). Bars represent total tumour volume with number of identified tumours indicated above each bar.
S8874	PLX5622 PLX5622是一种高选择性的CSF-1R抑制剂，IC50小于10 nM，其对CSF-1R的选择性比对KIT和FLT3的选择性高20倍以上。	J Neurochem, 2022, 10.1111/jnc.15581 J Neurosci, 2021, JN-RM-1502-21 Exp Cell Res, 2020, 396(2):112323
S0487	Sulfatinib Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib)是一种有效的、具有高度选择性的 tyrosine kinase 的抑制剂，对于 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 CSF1R 的IC50值分别为2 nM、24 nM、1 nM、15 nM和4 nM。Sulfatinib 在针对晚期NET患者的实验中显示出令人鼓舞的抗肿瘤活性和可控毒性。

目录号	产品描述	文献引用	实验数据
S1035	Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。	NPJ Breast Cancer,2022, 8(1):44 Hum Cell,2022, 10.1007/s13577-022-00671-y Cancer Cell,2021, S1535-6108(21)00659-0	Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S1003	Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635)是一种新型有效的ATP竞争性VEGFR/PDGFR抑制剂，作用于KDR，CSF-1R，Flt-1/3和PDGFRβ，其IC50分别为4 nM，3 nM，3 nM/4 nM和66 nM，对突变激酶依赖性癌细胞（即FLT3）最有效。Linifanib (ABT-869) 可诱导自噬和凋亡。Phase 3。	Hum Cell,2022, 10.1007/s13577-022-00671-y Cell Rep Med,2022, 3(1):100492 Cancer Lett,2021, 507:80-88	(B and C) KMCH-1 cells were plated alone (monoculture) or together with PDGF-BB-secreting LX-2 cells (co-culture) in a transwell insert co-culture system (KMCH-1 cells in the bottom wells and LX-2 cells in the inserts; 1:1 ratio) for 2 days. Cells were treated as indicated with vehicle, rhTRAIL (10 ng/ml for 6 h on day 2), rhTRAIL plus imatinib [rhTRAIL:10 ng/ml for 6 h on day 2; Imatinib: 5 μmol/L for 24 h (day2)], or rhTRAIL plus linifanib [rhTRAIL: 10 ng/ml for 6 h on day 2; Linifanib:0.5 μmol/L for 24 h (day2)]. After rhTRAIL treatment for 6 h,KMCH-1 cells were analysed for apoptotic nuclear morphology by DAPI-staining (B) and for DNA fragmentation by transferasemediated dUTP nick end labelling assay (C) with quantification of apoptotic nuclei by fluorescence microscopy.
S1181	ENMD-2076 ENMD-2076 选择性地作用于 Aurora A 和 Flt3，IC50分别为14 nM和1.86 nM，作用于Aurora A比作用于Aurora B选择性高25倍，对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα作用效果稍弱。ENMD-2076 可抑制各种人类实体瘤和造血癌细胞系的生长，其IC50值为0.025至0.7μM，可诱导凋亡和G2/M期停滞。Phase 2。	Cell,2021, 184(2):334-351.e20 Sci Adv,2021, 7(4)eabd7851 J Pediatr Hematol Oncol,2019, 41(6):e359-e370	Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
S1189	Aprepitant (MK-0869) Aprepitant (MK-0869, L-754030)是一种有效的选择性 neurokinin-1 receptor 拮抗剂，IC50为0.1 nM。Aprepitant 可降低炎症因子的表达水平，包括 G-CSF、IL-6、IL-8 和 TNFα。Aprepitant 可抑制人巨噬细胞 HIV 的感染。	Cancers (Basel),2021, 13(15)3871 Phytomedicine,2021, 95:153864 Nat Commun,2020, 29;11(1):2673	HepT1, HepG2, and HuH6 cells were treated with increasing doses of aprepitant or SP [100 nM] and Western blot analysis was performed for the apoptotic markers PARP, Caspase-3, and BID.
S1220	OSI-930 OSI-930是一种有效的Kit (c-Kit)， KDR和CSF-1R抑制剂，IC50分别为80 nM， 9 nM和15 nM，对Flt-1， c-Raf和Lck具有适度的抑制活性，对PDGFRα/β， Flt-3和Abl抑制活性较弱。Phase 1。	Cell Rep,2019, 28(9):2331-2344 Nat Biomed Eng,2018, 2(8):578-588 Mol Syst Biol,2015, 11(1):789	RE-luc2P-HEK293 cells were pretreated with 1uM OSI-930 (green), 20uM TBB (blue), 10uM CKI-7 (purple), or 10uM H-89 (orange) for 16 h and infected with Y. enterocolitica WA or Y. pestis Ind195 at MOI 1 and 20, respectively, for 1 h. Following stimulation with 10 ng/ml TNF-α at 5 h post-infection, luciferase activity was measured 24 h post-infection. Results were determined from two independent experiments performed in triplicate. A"*" denotes that the % NF-κβ inhibition using the inhibitors was significantly different (p<0.05) compared to the no drug control (black). The relative NF-κB inhibition by Yersinia infection was determined as a percentage of luciferase activity in bacteria-infected cells relative to luciferase activity in bacteria-free control cells.
S9620^New	Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) 是一种有效的 MET/CSF1R/SRC 抑制剂，IC50 分别为 0.14 nM、0.71 nM 和 0.12 nM。TPX-0022 在临床前模型中可调节肿瘤免疫微环境。
S3012	Pazopanib Pazopanib (GW786034) 是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms/CSF1R抑制剂，无细胞试验中IC50分别为10 nM，30 nM，47 nM，84 nM，74 nM，140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。	NPJ Breast Cancer,2022, 8(1):44 J Pharmacol Exp Ther,2022, 380(2):114-125 Birth Defects Res,2022, 10.1002/bdr2.2001	Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S8042	GW2580 GW2580 (SC-203877) 是一种选择性CSF-1R抑制剂，作用于c-FMS时，IC50为30 nM，比作用于b-Raf， CDK4， c-KIT， c-SRC， EGFR， ERBB2/4， ERK2， FLT-3， GSK3， ITK， JAK2等的选择性高150到500倍。	Brain Behav Immun,2021, S0889-1591(21)00097-0 Cardiovasc Res,2020, 10.1093/cvr/cvaa046 Neurobiol Dis,2020, 134:104705	CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, GW2580 (C) for 8 days. Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay.
S8015	Agerafenib (RXDX-105) Agerafenib (RXDX-105, CEP-32496) 是一种高度有效的BRAF(V600E/WT)和c-Raf抑制剂，K_d为14 nM/36 nM和39 nM，适度有效作用于Abl-1， c-Kit， RET (c-RET)， PDGFRβ和VEGFR2，对MEK-1， MEK-2， ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。	Mol Pharmacol,2021, 99(6):435-447 Dis Model Mech,2020, dmm.047779 Photodermatol Photoimmunol Photomed,2019, 10.1111/phpp.12520
S8721	PDGFR inhibitor 1 PDGFR inhibitor 1是一种具有口服活性的Kit (c-Kit)和PDGFR抑制剂，具有潜在的抗肿瘤活性。它还能抑制好几种其他激酶，包括VEGFR2、TIE2、PDGFR-beta和CSF1R，因此进而抑制肿瘤细胞的生长。	Oncogene,2022, 41(20):2860-2872
S7688	Ki20227 Ki20227 是一种口服活性的 c-Fms tyrosine kinase(CSF1R) 的高选择性抑制剂，对 c-Fms、vascular endothelial growth factor receptor-2 (KDR/VEGFR-2)、stem cell factor receptor (c-Kit) 和 platelet-derived growth factor receptor beta (PDGFRβ) 的IC50值为2 nM、12 nM、451 nM和217 nM。
S8401	Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂，具有潜在的抗肿瘤活性。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。	JCI Insight,2022, 7(7)e154824 Oncoimmunology,2022, 11(1):2021619 Hum Cell,2022, 10.1007/s13577-022-00671-y	E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493
S3570	ARRY-382 ARRY-382 是 CSF1R 的高选择性口服抑制剂，IC50 为 9 nM。
S8578	PRN1371 PRN1371是FGFR1-4的不可逆性共价抑制剂，对于FGFR1, 2, 3, 4和CSF1R的IC50分别为0.6、1.3、4.1、19.3、和8.1 nM。	Nat Commun,2021, 12(1):6572
S7725	BLZ945 BLZ945是一种具有口服活性的，有效的选择性 CSF-1R抑制剂，IC50为1 nM，比其最接近的受体酪氨酸激酶同系物高出1000多倍的选择性。	Proc Natl Acad Sci U S A,2022, 119(14):e2111804119 Cell Death Dis,2022, 13(2):166 Nat Commun,2021, 12(1):1858	CSF1R c.1085A>G genetic variant confers the sensitivity of macrophage survival to CSF-1R inhibitors. Macrophages differentiated from peripheral blood mononuclear cells were incubated with various concentrations of the CSF-1R inhibitor, BLZ945 (B) for 8 days Percentage of cell survival was determined by CellTiter-Glo® Luminescent Cell Viability Assay.
S7818	Pexidartinib (PLX3397) Pexidartinib (PLX3397)是一种口服有效的多靶点CSF-1R，Kit (c-Kit)，和 FLT3受体酪氨酸激酶抑制剂，其IC50分别为20 nM, 10 nM 和 160 nM。Pexidartinib (PLX3397) 可以诱导细胞凋亡和坏死，并具有抗肿瘤活性。Phase 3。	J Clin Invest,2022, 132(3)e145071 Aging Cell,2022, 10.1111/acel.13623 Int J Mol Sci,2022, 23(5)2793	(a) Reduced tumour burden in PLX3397 (PLX) treated mice relative to untreated (NT) (n=6, P=.015; unpaired t-test). Bars represent total tumour volume with number of identified tumours indicated above each bar.
S8874	PLX5622 PLX5622是一种高选择性的CSF-1R抑制剂，IC50小于10 nM，其对CSF-1R的选择性比对KIT和FLT3的选择性高20倍以上。	J Neurochem,2022, 10.1111/jnc.15581 J Neurosci,2021, JN-RM-1502-21 Exp Cell Res,2020, 396(2):112323
S0487	Sulfatinib Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib)是一种有效的、具有高度选择性的 tyrosine kinase 的抑制剂，对于 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 CSF1R 的IC50值分别为2 nM、24 nM、1 nM、15 nM和4 nM。Sulfatinib 在针对晚期NET患者的实验中显示出令人鼓舞的抗肿瘤活性和可控毒性。