c-RET

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抑制剂选择性比较

c-RET产品

所有产品 c-RET抑制剂(20)

目录号	产品描述	文献引用	实验数据
S1178	Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506)是一个多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR-β，Kit，RET和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。Regorafenib 可诱导自噬。	Front Oncol, 2020, 10:878 Antiviral Res, 2020, 178:104790 Arthritis Res Ther, 2020, 22(1):160	Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
S2736	Fedratinib (TG101348) Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。	PLoS Biol, 2020, 18(3):e3000646 Mol Ther Oncolytics, 2020, 30;17:169-179 J Interferon Cytokine Res, 2020, 40(2):92-105	Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
S1107	Danusertib (PHA-739358) Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。Phase 2。	Toxicol Sci, 2019, 10.1093/toxsci/kfz123 Drug Deliv Transl Res, 2019, doi: 101007/s13346-019-00668-5 Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211	Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
S1244	Amuvatinib (MP-470) Amuvatinib (MP-470)是一种有效的，作用于c-Kit、PDGFα和Flt3的多靶点抑制剂，IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。	Oncotarget, 2016, 7(15):19620-30 J Pathol, 2015, 237(1):14-24 Cancer Res, 2014, 74(20):5878-90	Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.
S1164	Lenvatinib (E7080) Lenvatinib (E7080)是一种多靶点抑制剂，无细胞试验中，作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效，IC50为4 nM/5.2，对VEGFR1/Flt-1作用效果稍弱，作用于VEGFR2/3比作用于FGFR1， PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、KIT和RET的抑制剂，并具有强效的抗肿瘤活性。Phase 3。	Cancers (Basel), 2020, 12(3) Cell Signal, 2020, 70:109573 J Hematol Oncol, 2020, 13(1):11	Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
S0377^New	CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) 是一种耐受性良好的、口服有效的、高选择性的 VEGFR-2 抑制剂，IC50值为40 nM。CS-2660（JNJ-38158471）还抑制紧密相关的酪氨酸激酶，如 Ret 和 Kit，IC50为180 nM和500 nM，但无明显活性 (>1 microM) 针对VEGFR-1和VEGFR-3。
S8781^New	Selpercatinib (LOXO-292) Selpercatinib (LOXO-292, ARRY-192)是一种有效、特异的RET抑制剂，对WT RET, RET (V804M), RET (V804L), RET (A883F), RET (M918T)和RET (S891A)的IC50值分别为1 nM、2 nM、2 nmM、4 nM、2 nM和2 nM。
S8716^New	Pralsetinib (BLU-667) Pralsetinib (BLU-667) 是一种高效的、选择性RET抑制剂，对WT RET的IC50值为0.4 nM。它对一些常见的RET致癌突变同样具有有效的抑制作用，IC50~0.4 nM。	Mol Cancer Res, 2020, 27;molcanres.1245.2019
S2692	TG101209 TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。	Nat Commun, 2018, 9(1):3259 Int Immunopharmacol, 2018, 54:354-365 Nat Commun, 2017, 8(1):1130	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
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， 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.
S8015	CEP-32496(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， PDGFRβ和VEGFR2，对MEK-1， MEK-2， ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。	Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520 Exp Gerontol, 2019, 126:110691 Nat Biomed Eng, 2018, 2(8):578-588
S8189	BAW2881 (NVP-BAW2881) BAW2881 (NVP-BAW2881)是一种新型的VEGFR酪氨酸激酶抑制剂。在1.0-4.3 nM浓度下能有效地抑制VEGFR1-3；在45-72 nM的浓度下，抑制PDGFRβ, c-Kit和RET。
S6520	WHI-P180 WHI-P180是多种激酶的抑制剂，对RET和KDR的IC50值分别为4.5 nM和66 nM。
S5240	lenvatinib Mesylate Lenvatinib Mesylate 是一种合成、具有口服活性的 tyrosine kinase 的抑制剂，可抑制血管内皮生长因子受体(VEGFR1-3)，成纤维细胞生长因子受体(FGFR1-4)，血小板衍生生长因子受体(PDGFRα)，干细胞因子受体(KIT)，并在转染过程中重新排列(RET)。甲磺酸来伐替尼具有潜在的抗肿瘤活性。	J Hematol Oncol, 2020, 13(1):11 ACS Appl Mater Interfaces, 2019, 101021/acsami9b20178 Animal Model Exp Med, 2019, 2(3):178-184
S8348	BMS-935177 BMS-935177是一种有效的、可逆的BTK抑制剂，IC50为2.8 nM，具有良好的激酶选择性。它对BTK比对其他激酶如TEC, BMX, ITK, and TXK更有效力，选择性是其5-67倍。
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、CSF-1R、PDGFR-α/PDGFR-β、FLT4、KIT和VEGFR-2并可诱导细胞凋亡。	Cancers (Basel), 2020, 26;12(6):E1366 Cancer Immunol Res, 2019, 7(9):1457-1471 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104	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
S8518	AD80 AD80，一种多激酶抑制剂，对人源RET、BRAF、S6K和SRC活性较强，但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。	Mol Cancer Res, 2020, 27;molcanres.1245.2019
S8696	2-D08 2-D08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, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。
S8821	GSK3179106 GSK3179106是有效的、选择性的RET kinase抑制剂，IC50为0.3 nM。
S5077	Regorafenib Monohydrate Regorafenib 瑞戈非尼是一种新型口服的多重激酶抑制剂，对VEGFR1、小鼠VEGFR2、小鼠VEGFR3、PDGFR-β、KIT、RET、RAF-1、B-RAF和B-RAF(V600E)的IC50分别为13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM。	Front Oncol, 2020, 10:878 Antiviral Res, 2020, 178:104790 Arthritis Res Ther, 2020, 22(1):160

目录号	产品描述	文献引用	实验数据
S1178	Regorafenib (BAY 73-4506) Regorafenib (BAY 73-4506)是一个多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR-β，Kit，RET和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。Regorafenib 可诱导自噬。	Front Oncol,2020, 10:878 Antiviral Res,2020, 178:104790 Arthritis Res Ther,2020, 22(1):160	Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
S2736	Fedratinib (TG101348) Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。	PLoS Biol,2020, 18(3):e3000646 Mol Ther Oncolytics,2020, 30;17:169-179 J Interferon Cytokine Res,2020, 40(2):92-105	Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
S1107	Danusertib (PHA-739358) Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。Phase 2。	Toxicol Sci,2019, 10.1093/toxsci/kfz123 Drug Deliv Transl Res,2019, doi: 101007/s13346-019-00668-5 Leuk Lymphoma,2019, 10.1080/10428194.2019.1594211	Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
S1244	Amuvatinib (MP-470) Amuvatinib (MP-470)是一种有效的，作用于c-Kit、PDGFα和Flt3的多靶点抑制剂，IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。	Oncotarget,2016, 7(15):19620-30 J Pathol,2015, 237(1):14-24 Cancer Res,2014, 74(20):5878-90	Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.
S1164	Lenvatinib (E7080) Lenvatinib (E7080)是一种多靶点抑制剂，无细胞试验中，作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效，IC50为4 nM/5.2，对VEGFR1/Flt-1作用效果稍弱，作用于VEGFR2/3比作用于FGFR1， PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、KIT和RET的抑制剂，并具有强效的抗肿瘤活性。Phase 3。	Cancers (Basel),2020, 12(3) Cell Signal,2020, 70:109573 J Hematol Oncol,2020, 13(1):11	Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
S0377^New	CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) 是一种耐受性良好的、口服有效的、高选择性的 VEGFR-2 抑制剂，IC50值为40 nM。CS-2660（JNJ-38158471）还抑制紧密相关的酪氨酸激酶，如 Ret 和 Kit，IC50为180 nM和500 nM，但无明显活性 (>1 microM) 针对VEGFR-1和VEGFR-3。
S8781^New	Selpercatinib (LOXO-292) Selpercatinib (LOXO-292, ARRY-192)是一种有效、特异的RET抑制剂，对WT RET, RET (V804M), RET (V804L), RET (A883F), RET (M918T)和RET (S891A)的IC50值分别为1 nM、2 nM、2 nmM、4 nM、2 nM和2 nM。
S8716^New	Pralsetinib (BLU-667) Pralsetinib (BLU-667) 是一种高效的、选择性RET抑制剂，对WT RET的IC50值为0.4 nM。它对一些常见的RET致癌突变同样具有有效的抑制作用，IC50~0.4 nM。	Mol Cancer Res,2020, 27;molcanres.1245.2019
S2692	TG101209 TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。	Nat Commun,2018, 9(1):3259 Int Immunopharmacol,2018, 54:354-365 Nat Commun,2017, 8(1):1130	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
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， 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.
S8015	CEP-32496(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， PDGFRβ和VEGFR2，对MEK-1， MEK-2， ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。	Photodermatol Photoimmunol Photomed,2019, 10.1111/phpp.12520 Exp Gerontol,2019, 126:110691 Nat Biomed Eng,2018, 2(8):578-588
S8189	BAW2881 (NVP-BAW2881) BAW2881 (NVP-BAW2881)是一种新型的VEGFR酪氨酸激酶抑制剂。在1.0-4.3 nM浓度下能有效地抑制VEGFR1-3；在45-72 nM的浓度下，抑制PDGFRβ, c-Kit和RET。
S6520	WHI-P180 WHI-P180是多种激酶的抑制剂，对RET和KDR的IC50值分别为4.5 nM和66 nM。
S5240	lenvatinib Mesylate Lenvatinib Mesylate 是一种合成、具有口服活性的 tyrosine kinase 的抑制剂，可抑制血管内皮生长因子受体(VEGFR1-3)，成纤维细胞生长因子受体(FGFR1-4)，血小板衍生生长因子受体(PDGFRα)，干细胞因子受体(KIT)，并在转染过程中重新排列(RET)。甲磺酸来伐替尼具有潜在的抗肿瘤活性。	J Hematol Oncol,2020, 13(1):11 ACS Appl Mater Interfaces,2019, 101021/acsami9b20178 Animal Model Exp Med,2019, 2(3):178-184
S8348	BMS-935177 BMS-935177是一种有效的、可逆的BTK抑制剂，IC50为2.8 nM，具有良好的激酶选择性。它对BTK比对其他激酶如TEC, BMX, ITK, and TXK更有效力，选择性是其5-67倍。
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、CSF-1R、PDGFR-α/PDGFR-β、FLT4、KIT和VEGFR-2并可诱导细胞凋亡。	Cancers (Basel),2020, 26;12(6):E1366 Cancer Immunol Res,2019, 7(9):1457-1471 Clin Cancer Res,2019, 10.1158/1078-0432.CCR-19-1104	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
S8518	AD80 AD80，一种多激酶抑制剂，对人源RET、BRAF、S6K和SRC活性较强，但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。	Mol Cancer Res,2020, 27;molcanres.1245.2019
S8696	2-D08 2-D08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, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。
S8821	GSK3179106 GSK3179106是有效的、选择性的RET kinase抑制剂，IC50为0.3 nM。
S5077	Regorafenib Monohydrate Regorafenib 瑞戈非尼是一种新型口服的多重激酶抑制剂，对VEGFR1、小鼠VEGFR2、小鼠VEGFR3、PDGFR-β、KIT、RET、RAF-1、B-RAF和B-RAF(V600E)的IC50分别为13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM。	Front Oncol,2020, 10:878 Antiviral Res,2020, 178:104790 Arthritis Res Ther,2020, 22(1):160

研究领域

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c-RET

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研究领域

抑制剂选择性比较

c-RET产品