Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6409 |
ALK kinase inhibitor-1
SAR348830 |
Others | Others |
SAR348830 是间变性淋巴瘤激酶ALK 抑制剂。 | |||
T10285 |
ALK inhibitor 1
|
FAK; IGF-1R; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
ALK inhibitor 1 是嘧啶类 ALK 的有效抑制剂。它是一种睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2;IC50=31 nM) 和粘着斑激酶 (FAK;IC50=2 nM) 抑制剂。 | |||
T11184 |
EML4-ALK kinase inhibitor 1
EML4 ALK kinase inhibitor 1,EML4-ALK kinase inhibitor 1 |
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) 是有效的、具有口服活性的类棘皮细胞微管相关蛋白4-间变性淋巴瘤激酶 (EML4-ALK) 的抑制剂,其 IC50 值为 1 nM。 | |||
T3059 |
ALK-IN-1
AP26113,Brigatinib,AP26113-analog |
EGFR; IGF-1R; ALK | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
ALK-IN-1 (AP26113) 是一种高效的、选择性的 ALK 激酶抑制剂。 | |||
T11254 |
F-1
|
ROS; ALK; ROS Kinase | Angiogenesis; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
F-1 是 ALK 和 ROS1 的双重抑制剂,抑制 ALK 的磷酸化及下游通路,可作用于对 ALKWT (IC50:2.1 nM),ROS1WT (IC50:2.3 nM),ALKL1196M (IC50:1.3 nM) 和 ALKG1202R (IC50:3.9 nM)。 | |||
T4015 |
HG-14-10-04
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
HG-14-10-04 是一种特异的 ALK 抑制剂,IC50=20 nM。 | |||
T2641 |
KRCA-0008
KRCA 0008,KRCA0008 |
ACK; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
KRCA-0008 是高效的、选择性的 ALK/Ack1 抑制剂,对ALK 和Ack1的IC50值分别为12nM 和4nM,显示出非hERG 依赖性药物活性。 | |||
T16708 |
R-268712
|
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
R-268712 是选择性的 ALK5 抑制剂(IC50:2.5 nM)。 | |||
T2251 |
NVP-TAE 684
TAE684,5-氯-N2-[2-甲氧基-4-[4-(4-甲基-1-哌嗪基)-1-哌啶基]苯基]-N4-[2-[(1-甲基乙基)磺酰基]苯基]-2,4-嘧啶二胺 |
Apoptosis; ALK | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
NVP-TAE 684 (TAE684) 是一种高效特异性 ALK 抑制剂,阻止 ALCL 衍生的 ALK 依赖性细胞株的生长,IC50值为 3 nM。 | |||
T67699L |
ALK/ROS1 inhibitor 2e HCL
(R)-1-(2-((2-methoxy-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(trifluoromethoxy)benzyl)piperidine-3-carboxamide hydrochloride(2365497-12-5 Free base) |
Apoptosis | Apoptosis |
ALK/ROS1 inhibitor 2e HCL 具有抗凋亡、抗增殖和抗肿瘤活性。 | |||
T1936 |
Alectinib
阿来替尼,RG-7853,艾乐替尼,AF802,CH5424802,AF-802 |
VEGFR; Tyrosine Kinases; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
Alectinib (RG-7853) 是一种有效的、选择性的、口服具有活力的、ATP 竞争性的 ALK 抑制剂,其 IC50=1.9 nM,Kd=2.4 nM,并且还抑制 ALK F1174L 和 ALK R1275Q,其 IC50分别为 1 nM 和 3.5 nM。它还有中枢神经系统渗透能力。 | |||
T8387 |
Alectinib hydrochloride
艾乐替尼盐酸盐,CH5424802 (Hydrochloride),AF-802 (Hydrochloride),RO5424802 (Hydrochloride) |
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
Alectinib hydrochloride (RO5424802 Hydrochloride) 是一种有效的、选择性的、口服具有活力的、ATP 竞争性的 ALK 抑制剂,其IC50=1.9 nM,Kd=2.4 nM,并且还抑制ALK F1174L 和ALK R1275Q,其IC50分别为 1 nM 和 3.5 nM。它还有中枢神经系统渗透能力。 | |||
T3678 |
Entrectinib
RXDX-101,恩曲替尼,NMS-E628 |
Trk receptor; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂,具有抗肿瘤和中枢神经活性,抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。 | |||
T3061 |
Lorlatinib
劳拉替尼,PF-6463922,PF-06463922,Loratinib |
Apoptosis; Tyrosine Kinases; ROS; ALK; ROS Kinase | Angiogenesis; Apoptosis; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Lorlatinib (PF-6463922) 是一种具有口服活性,选择性,脑渗透性和 ATP 竞争性的ROS1/ALK 抑制剂,具有抗癌活性。它对 ROS1、野生型 ALK 和 ALKL1196M 的Ki 值分别为 <0.025 nM、<0.07 nM 和 0.7 nM。 | |||
T8399 |
Crizotinib hydrochloride
克里唑替尼盐酸,PF-02341066 hydrochloride |
c-Met/HGFR; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Crizotinib hydrochloride (PF-02341066 hydrochloride) 是一种可口服的,具有选择性的 ATP 竞争性双 ALK 和 c-Met 抑制剂。它也是 ROS 原癌基因 1 抑制剂,可抑制肿瘤生长。在细胞的实验中,它抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化。 | |||
T10286 | ALK/ROS1-IN-1 | Others | Others |
ALK/ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK/ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme). | |||
T83146 |
ALK-IN-27
|
||
ALK-IN-27(化合物1)是一种有效的ALK抑制剂,展现出抗肿瘤活性。在Ba/F3 CLIP1-LTK细胞中,ALK-IN-27的IC50为2.7 nM。 | |||
T61443 | Trk-IN-7 | ||
Trk-IN-7 (compound I-6) is a highly potent inhibitor of TRK, exhibiting IC50 values ranging from 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. In addition, Trk-IN-7 demonstrates notable inhibition against EML4-ALK (IC50 <15 nM), as well as ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50 = 5-50 nM) [1]. | |||
T73417 | Con B-1 | ||
ConB-1是一种对正常细胞低毒的强选择性 ALK 抑制剂。 | |||
T72931 | TRK/ALK-IN-1 | ||
TRK/ALK-IN-1 是一种有效的 TRK 和 ALK 双重抑制剂。TRK/ALK-IN-1 在酶促测定中与抗增殖活性非常吻合,对 TRKA、ALKIC50值分别为 2.2、9.3 和 38 nM< sup>WT 和 ALKL1196M。TRK/ALK-IN-1具有研究癌症疾病的潜力。 | |||
T79392 | ALK/EGFR-IN-1 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
ALK/EGFR-IN-1(Compound 8l)是一款高效的ALK/EGFR双重抑制剂,专门针对EGFR和ALK的磷酸化过程进行抑制。该化合物对H1975细胞内的EGFRL858R/T790M突变体和BaF3细胞内的EML4-ALK表达类型表现出优异的抑制活性,其IC50值分别为4.3 nM和3.6 nM。ALK/EGFR-IN-1用于非小细胞肺癌(NSCLC)的科学研究具有重要应用价值。 | |||
T79394 | ALK/EGFR-IN-3 | ||
ALK/EGFR-IN-3 为ALK与EGFR的强效双重抑制剂,有效遏制H1975、PC9以及Baf3-EML4-ALK癌细胞系的生长,其IC50值分别为0.1360、0.0332及0.0339 μM。 | |||
T79393 | ALK/EGFR-IN-2 | ||
ALK/EGFR-IN-2 是一种高效的 ALK 和 EGFR 双重抑制剂,能够诱导癌细胞凋亡及 G0/G1 细胞周期停滞。此化合物在 H1975、PC9 和 Baf3-EML4-ALK 癌熙胞株的增殖抑制实验中,其 IC50 值分别为0.0034、0.0065 和 0.0018 μM,表明其对这些癌熙胞系具有显著的抑制作用。 | |||
T74522 | ALK-IN-21 | ||
ALK-IN-21(Compound B10)是一款高效的ALK抑制剂,其针对ALKWT、ALKL1196M和ALKG1202R的IC50值依次为4.59 nM、2.07 nM和5.95 nM。该化合物能显著抑制ALK阳性的Karpas299与H2228细胞系的增殖,均展现出0.07 μM的IC50值。ALK-IN-21主要用于研究间变性大细胞淋巴瘤。 | |||
T70060 |
PF-06463922 acetate
|
||
PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC). | |||
T9414 |
TPX-0131
|
||
TPX-0131 是一种有效、选择性、CNS 渗透性和口服活性的野生型ALK 抑制剂 (IC50为 1.4 nM) 并且有效对抗 ALK 耐药突变,例如G1202R(IC50为 0.3 nM)、L1196M(IC50为 0.3 nM)。TPX-0131 具有很强的抗肿瘤活性。 | |||
T62613 |
ALK5-IN-26
|
||
ALK5-IN-26 (EX-22) 是一种 ALK(Activin receptor-like kinase) 的抑制剂。ALK5-IN-26 对 ALK5 (IC50≤1 nM) 具有抑制作用。ALK5-IN-26 能够用于研究癌症。 | |||
T38584 |
ALK-IN-12
|
||
ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy. | |||
T79363 | APG-2449 | ROS Kinase | Tyrosine Kinase/Adaptors |
APG-2449为口服活性的ALK/ROS1/FAK抑制剂,在非小细胞肺癌(NSCLC)的小鼠模型中显示出显著的抗肿瘤效果。 | |||
T83856 |
AP-1
|
||
AP-1是一种微型化的蛋白质水解靶向嵌合体(PROTAC),由吲哚美辛(±)连接的间变性淋巴瘤激酶(ALK)配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时,AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK,此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变(ALKF1174L)的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性(IC50 = 0.1265 nM),但对非ALK依赖的THP-1细胞无细胞毒性(IC50 = 2,704 nM)。在给药剂量为25, 50, 和100 mg/kg时,能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。 | |||
T37585 | Ensartinib | ||
Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring N... | |||
T61872 |
Trk-IN-10
|
||
Trk-IN-10 (Compound 14j) is a highly effective inhibitor of TRK, with an IC50 of 0.86 nM against TrkA and 6.92 nM against TrkA G595R. As an RTK, Trk plays a crucial role as a drug target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) demonstrates superior selectivity in inhibiting Trk, which has potential implications for toxicity reduction [1]. |