CSF-1R
CSF-1R产品
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。 |
![]() ![]() 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。 |
![]() ![]() (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-2076ENMD-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。 |
![]() ![]() Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
|
|
S1189 |
AprepitantAprepitant (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。 |
![]() ![]() 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-930OSI-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。 |
![]() ![]() 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.
|
|
S7688New |
Ki20227Ki20227 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。 |
||
S0487New |
SulfatinibSulfatinib 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。 |
||
S3012 |
PazopanibPazopanib (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。 |
![]() ![]() 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 |
GW2580GW2580 (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。 |
![]() ![]() 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,Kd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。 |
||
S8721 |
PDGFR inhibitor 1PDGFR 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。 |
||
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。 |
![]() ![]() 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 |
|
S8578 |
PRN1371PRN1371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。 |
||
S7725 |
BLZ945BLZ945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。 |
![]() ![]() 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。 |
![]() ![]() (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 |
PLX5622PLX5622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。 |
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。 |
![]() ![]() 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。 |
![]() ![]() (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-2076ENMD-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。 |
![]() ![]() Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
|
|
S1189 |
AprepitantAprepitant (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。 |
![]() ![]() 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-930OSI-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。 |
![]() ![]() 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.
|
|
S7688New |
Ki20227Ki20227 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。 |
||
S0487New |
SulfatinibSulfatinib 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。 |
||
S3012 |
PazopanibPazopanib (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。 |
![]() ![]() 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 |
GW2580GW2580 (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。 |
![]() ![]() 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,Kd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。 |
||
S8721 |
PDGFR inhibitor 1PDGFR 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。 |
||
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。 |
![]() ![]() 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 |
|
S8578 |
PRN1371PRN1371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。 |
||
S7725 |
BLZ945BLZ945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。 |
![]() ![]() 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。 |
![]() ![]() (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 |
PLX5622PLX5622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。 |