ROS1

抑制剂选择性比较

ROS1产品

所有产品 ROS1抑制剂(8)

目录号	产品描述	文献引用	实验数据
S1068	Crizotinib (PF-02341066) Crizotinib (PF-02341066) 克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。	Cancer Cell, 2020, 13;37(1):104-122e12 Nat Commun, 2020, 25;11(1):1556 Sci Adv, 2020, 22;6(21):eaaz8521	(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). P < 0.005, *P < 0.001 (Student^,s t test).
S8901^New	DS-6051b DS-6051b是新一代的选择性的ROS1/NTRK 抑制剂，对ROS1，TrkA，TrkB 和TrkC的ic50分别为0.207 nM，0.622 nM，2.28 nM和0.980 nM。
S7014	Merestinib (LY2801653) Merestinib (LY2801653) 是一种2型ATP竞争型的慢抑制剂，抑制MET酪氨酸激酶，Ki值为2 nM。药效的停留时间为0.00132 min(-1)，t_^1/2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
S7998	Entrectinib (RXDX-101) Entrectinib (RXDX-101, NMS-E628) 是一种口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制剂，IC50范围为 0.1~1.7 nM。Entrectinib (RXDX-101) 可诱导自噬。Phase 2。	Clin Cancer Res, 2020, 8 Cancer Discov, 2020, 1 pii: CD-19-1030 Lung Cancer, 2020, 144:20-29	Tumor cells were treated with entrectinib (10 nmol/L) for 4 hours or c-PARP for 48 hours, and harvested lysates were assessed by Western blotting. Data shown are representative of three independent experiments with similar results.
S8583	Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) 是一种新型的ALK/ROS1/TRK抑制剂，对WT ALK、ALK(G1202R)、ALK(L1196M)的IC50分别为1.01 nM、1.26 nM、1.08 nM；同时也是一种有效的SRC抑制剂，IC50为5.3 nM。	NPJ Precis Oncol, 2020, 4:21
S8229	Brigatinib (AP26113) Brigatinib (AP26113) 是一种有效的、选择性的ALK抑制剂，IC50=0.6 nM；也是ROS1抑制剂，IC50=0.9 nM。它还能以相对较低的效力抑制IGF-1R、FLT3、FLT3(D835Y)和EGFR。	Sci Signal, 2020, 26;13(633):eaba3176 Cell Syst, 2019, 8(2):97-108 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104	Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
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, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。
S7536	Lorlatinib (PF-6463922) PF-06463922 是一个强效的，双重 ALK/ROS1 的抑制剂，对ROS1, ALK (WT), 以及ALK (L1196M)的K_i分别为<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可诱导凋亡。Phase 1。	Clin Cancer Res, 2020, 8 Cancer Discov, 2020, 1 pii: CD-19-1030 Lung Cancer, 2020, 144:20-29	Sub-G1 and cell cycle phase distribution of NBLW and NBLW-R cells treated for 24 hours with DMSO, 1× or 10× the respective GI 50 concentrations of PF-06463922.

目录号	产品描述	文献引用	实验数据
S1068	Crizotinib (PF-02341066) Crizotinib (PF-02341066) 克唑替尼是一种有效的c-Met和ALK抑制剂，在细胞试验中IC50分别为11 nM 和 24 nM。它同时也是有效的ROS1抑制剂，其Ki值小于0.025 nM。Crizotinib可在多种肺癌细胞系中通过抑制STAT3通路来诱导自噬。	Cancer Cell,2020, 13;37(1):104-122e12 Nat Commun,2020, 25;11(1):1556 Sci Adv,2020, 22;6(21):eaaz8521	(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). P < 0.005, *P < 0.001 (Student^,s t test).
S8901^New	DS-6051b DS-6051b是新一代的选择性的ROS1/NTRK 抑制剂，对ROS1，TrkA，TrkB 和TrkC的ic50分别为0.207 nM，0.622 nM，2.28 nM和0.980 nM。
S7014	Merestinib (LY2801653) Merestinib (LY2801653) 是一种2型ATP竞争型的慢抑制剂，抑制MET酪氨酸激酶，Ki值为2 nM。药效的停留时间为0.00132 min(-1)，t_^1/2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
S7998	Entrectinib (RXDX-101) Entrectinib (RXDX-101, NMS-E628) 是一种口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制剂，IC50范围为 0.1~1.7 nM。Entrectinib (RXDX-101) 可诱导自噬。Phase 2。	Clin Cancer Res,2020, 8 Cancer Discov,2020, 1 pii: CD-19-1030 Lung Cancer,2020, 144:20-29	Tumor cells were treated with entrectinib (10 nmol/L) for 4 hours or c-PARP for 48 hours, and harvested lysates were assessed by Western blotting. Data shown are representative of three independent experiments with similar results.
S8583	Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) 是一种新型的ALK/ROS1/TRK抑制剂，对WT ALK、ALK(G1202R)、ALK(L1196M)的IC50分别为1.01 nM、1.26 nM、1.08 nM；同时也是一种有效的SRC抑制剂，IC50为5.3 nM。	NPJ Precis Oncol,2020, 4:21
S8229	Brigatinib (AP26113) Brigatinib (AP26113) 是一种有效的、选择性的ALK抑制剂，IC50=0.6 nM；也是ROS1抑制剂，IC50=0.9 nM。它还能以相对较低的效力抑制IGF-1R、FLT3、FLT3(D835Y)和EGFR。	Sci Signal,2020, 26;13(633):eaba3176 Cell Syst,2019, 8(2):97-108 Clin Cancer Res,2019, 10.1158/1078-0432.CCR-19-1104	Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
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, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。
S7536	Lorlatinib (PF-6463922) PF-06463922 是一个强效的，双重 ALK/ROS1 的抑制剂，对ROS1, ALK (WT), 以及ALK (L1196M)的K_i分别为<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可诱导凋亡。Phase 1。	Clin Cancer Res,2020, 8 Cancer Discov,2020, 1 pii: CD-19-1030 Lung Cancer,2020, 144:20-29	Sub-G1 and cell cycle phase distribution of NBLW and NBLW-R cells treated for 24 hours with DMSO, 1× or 10× the respective GI 50 concentrations of PF-06463922.