c-RET

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研究领域

抑制剂选择性比较

c-RET产品

所有产品 c-RET抑制剂(13) 新c-RET产品

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。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Nat Cell Biol, 2019, 21(2):203-213	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
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。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).
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).
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^New	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。
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	BLU-667 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。
S8821^New	GSK3179106 GSK3179106是有效的、选择性的RET kinase抑制剂，IC50为0.3 nM。
S5248	Apatinib Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.	Cell Death Dis, 2019, 10(10):784 Oxid Med Cell Longev, 2019, 2019:5152072 Cancer Cell Int, 2019, 19:117
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。
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。
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。
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。

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。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Nat Cell Biol,2019, 21(2):203-213	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
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。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).
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).
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^New	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。
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	BLU-667 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。
S8821^New	GSK3179106 GSK3179106是有效的、选择性的RET kinase抑制剂，IC50为0.3 nM。
S5248	Apatinib Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.	Cell Death Dis,2019, 10(10):784 Oxid Med Cell Longev,2019, 2019:5152072 Cancer Cell Int,2019, 19:117
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。
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。
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。
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。