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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。
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。
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。
T11254 F-1

ROS; ALK; ROS Kinase Angiogenesis; Immunology/Inflammation; Tyrosine Kinase/Adaptors
F-1ALK 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)。
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。
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。
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。
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 ALKALKL1196M 的Ki 值分别为 <0.025 nM、<0.07 nM 和 0.7 nM。
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、ROS1ALK 抑制剂,具有抗肿瘤和中枢神经活性,抑制 TrkA、TrkB、TrkC、ROS1ALK 的 IC50值分别为 1、3、5、12 和 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。
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。
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).
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.
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。

化合物

ALK kinase inhibitor-1
Cat.No: T6409
Synonym: SAR348830
Target: Others
EML4-ALK kinase inhibitor 1
Cat.No: T11184
Synonym: EML4 ALK kinase inhibitor 1,EML4-​ALK kinase inhibitor 1
Target: ALK
ALK inhibitor 1
Cat.No: T10285
Synonym:
Target: FAK, IGF-1R, ALK
F-1
Cat.No: T11254
Synonym:
Target: ROS, ALK, ROS Kinase
ALK-IN-1
Cat.No: T3059
Synonym: AP26113,Brigatinib,AP26113-analog
Target: EGFR, IGF-1R, ALK
HG-14-10-04
Cat.No: T4015
Synonym:
Target: ALK
KRCA-0008
Cat.No: T2641
Synonym: KRCA 0008,KRCA0008
Target: ACK, ALK
R-268712
Cat.No: T16708
Synonym:
Target: ALK, TGF-beta/Smad
NVP-TAE 684
Cat.No: T2251
Synonym: 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
Target: Apoptosis, ALK
Alectinib
Cat.No: T1936
Synonym: 阿来替尼,RG-7853,艾乐替尼,AF802,CH5424802,AF-802
Target: VEGFR, Tyrosine Kinases, ALK
Lorlatinib
Cat.No: T3061
Synonym: 劳拉替尼,PF-6463922,PF-06463922,Loratinib
Target: Apoptosis, Tyrosine Kinases, ROS, ALK, ROS Kinase
Entrectinib
Cat.No: T3678
Synonym: RXDX-101,恩曲替尼,NMS-E628
Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase
Crizotinib hydrochloride
Cat.No: T8399
Synonym: 克里唑替尼盐酸,PF-02341066 hydrochloride
Target: c-Met/HGFR, ROS, ALK, Autophagy, ROS Kinase
ALK5-IN-26
Cat.No: T62613
Synonym:
Target:
PF-06463922 acetate
Cat.No: T70060
Synonym:
Target:
ALK-IN-12
Cat.No: T38584
Synonym:
Target:
AP-1
Cat.No: T83856
Synonym:
Target:
TargetMol Loading
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