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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。 | |||
T3079 |
GSK1838705A
|
IGF-1R; JNK; S6 Kinase; ALK | Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
GSK1838705A 是一种高效的、可逆的IGF-IR (IC50:2.0 nM) 和胰岛素受体 (IC50:1.6 nM)抑制剂,也可抑制ALK (IC50:0.5 nM)。 | |||
T15612 |
JH-VIII-157-02
|
Microtubule Associated; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
JH-VIII-157-02 是一种 ALK 抑制剂,可抑制棘皮动物微管相关蛋白样 4-ALK (EML4-ALK),对EML4-ALK G1202R、EML4-ALKwt、EML4-ALK C1156Y、EML4-ALK F1174L 和 EML4-ALK F1174L 的 IC50 均为 2 nM。 | |||
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)。 | |||
T16153 |
MS4078
|
ALK; PROTACs | Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors |
MS4078 是一种基于 Cereblon 配体的间变性淋巴瘤激酶 PROTAC ,结合 ALK 的 Kd 为 19 nM。 | |||
T1962 |
ASP3026
ASP 3026 |
Apoptosis; ALK | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
ASP3026 是一种选择性的,具有口服活性的间变性淋巴瘤激酶抑制剂,可诱导肿瘤细胞凋亡,可研究非小细胞肺癌。 | |||
T3041 |
ALK inhibitor 2
|
FAK; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
ALK inhibitor 2 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=37 nM) 和粘着斑激酶 (FAK;IC50=5 nM) 抑制剂。 | |||
T4257 |
Belizatinib
TSR-011 |
Trk receptor; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
Belizatinib (TSR-011) 是可口服的ALK 和 TRKA、TRKB、TRKC 双重抑制剂,对野生型重组 ALK 的IC50值为0.7 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。 | |||
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。 | |||
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。 | |||
T1967 |
AZD-3463
ALK/IGF1R inhibitor |
Apoptosis; IGF-1R; ALK; Autophagy | Angiogenesis; Apoptosis; Autophagy; Tyrosine Kinase/Adaptors |
AZD-3463 (ALK/IGF1R inhibitor) 是一种具有口服活性的ALK/IGF1R 抑制剂,对 ALK 作用的Ki 值为 0.75 nM。它可诱导神经母细胞瘤细胞凋亡和自噬。 | |||
T3621 |
Brigatinib
布格替尼,AP-26113 |
EGFR; FLT; ROS; IGF-1R; ALK | Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Brigatinib (AP-26113) 是一种有效,选择性的ALK 抑制剂 (IC50:0.6 nM)。 | |||
T4071 |
Repotrectinib
TPX-0005,TPX 0005,TPX0005 |
Trk receptor; ROS; Src; ALK; ROS Kinase | Angiogenesis; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Repotrectinib (TPX-0005) 是ROS1(IC50=0.07 nM) 和TRK(对 TRKA/B/C 的IC50=0.83/0.05/0.1 nM) 抑制剂,能够抑制 WTALK(IC50=1.01 nM)。它具有抗癌作用。 | |||
T1791 |
Ceritinib
色瑞替尼,LDK378 |
Serine Protease; IGF-1R; ALK | Angiogenesis; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
Ceritinib (LDK378) 是一种选择性,具有口服活性的、ATP 竞争性的 ALK 酪氨酸激酶抑制剂,IC50=200 pM。 它还抑制 IGF-1R (IC50:8 nM),InsR (IC50:7 nM) 和 STK22D (IC50:23 nM)。它显示出良好抗肿瘤效力。 | |||
T1661 |
Crizotinib
PF-02341066,克唑替尼 |
c-Met/HGFR; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Crizotinib (PF-02341066) 是一种小分子酪氨酸激酶抑制剂,抑制 c-MET 和 ALK 受体 (IC50=8/20 nM),具有 ATP 竞争性,也可以抑制 ROS1。Crizotinib 具有抗肿瘤活性,可以抑制肿瘤生长。 | |||
T3550 |
X-376
Ensartinib,X-396,恩沙替尼 |
c-Met/HGFR; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
X-376 (Ensartinib) 是一种有效的ALK 抑制剂,对许多具有crizotinib 抗性的ALK 突变型和中枢神经系统转移具有高活性。它能有效地抑制野生型ALK 和ALK 变体(F1174, C1156Y, L1196M, S1206R, T1151和G1202R 突变型),IC50小于4 nM。 | |||
T2655 |
CEP-37440
CEP37440 |
FAK; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
CEP-37440 是一种新型的 FAK (IC50:2.3 nM) 和 ALK (IC50:120 nM) 双重抑制剂。 | |||
T13416 |
ZX-29
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
ZX-29 是一种选择性ALK 抑制剂,对ALK、ALK L1196M 和ALK G1202R 的IC50分别为 2.1 nM、1.3 nM 和 3.9 nM。它还可诱导保护性自噬并具有抗肿瘤作用。它通过诱导内质网应激来诱导细胞凋亡,并克服了由ALK 突变引起的细胞抗性。 | |||
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。 | |||
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。 | |||
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。 | |||
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)。 | |||
T1791L |
Ceritinib dihydrochloride
LDK378 dihydrochloride,双盐酸盐色瑞替尼 |
IGF-1R; ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
Ceritinib dihydrochloride (LDK378 dihydrochloride) 是一种选择性的、口服具有活性的、ATP 竞争性的ALK 酪氨酸激酶抑制剂 (IC50:200 pM)。它还抑制IGF-1R (IC50:8 nM),InsR (IC50:7 nM) 和 STK22D (IC50:23 nM)。它显示出良好的抗肿瘤作用。 | |||
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。 | |||
T22324 |
Ensartinib hydrochloride
Ensartinib dihydrochloride,X-396 dihydrochloride |
Others; Trk receptor; c-Met/HGFR; ALK | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
Ensartinib hydrochloride (X-396 dihydrochloride) 是双重的 ALK/MET 抑制剂,IC50分别 <0.4 nM 和 0.74 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。 | |||
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。 | |||
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。 | |||
T2612 |
CEP-28122
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
CEP28122 是一种高效的、选择性的 ALK 抑制剂 (IC50:1.9 ± 0.5 nM)。 | |||
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。 | |||
T13781 |
MS4077
|
ALK; PROTACs | Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors |
MS4077 is an degrader of anaplastic lymphoma kinase (ALK) PROTAC(Kd of 37 nM for binding affinity to ALK). | |||
T10283 |
ALK-IN-5
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK, IC50: 2.9 nM). | |||
T73189 |
Ficonalkib
|
Others | Others |
Ficonalkib, 作为间变性淋巴瘤激酶(ALK)的有效抑制剂,其作用目标是酪氨酸激酶受体,可用于抗肿瘤药物的开发。 | |||
T70060 |
PF-06463922 acetate
|
Others | Others |
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
|
Others | Others |
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. | |||
T72317 |
CEP-28122 mesylate salt
|
Others | Others |
CEP-28122 mesylate salt 是一种二氨基嘧啶衍生物,是一种高度有效的选择性且具有口服活性的ALK 抑制剂,对重组 ALK 激酶活性的IC50为 1.9 nM。CEP-28122 在人类癌症的 ALK 阳性实验模型中具有抗肿瘤活性。 CEP-28122 具有良好的药效药代活性。 | |||
T37084 |
TL13-22
TL 13-22 |
Others | Others |
Negative control for TL 13-12 . Displays no degradation of ALK in cell lines. Highly potent inhibitor of ALK (IC50 = 0.54 nM) Powell et al (2018) Chemically induced degradation of anaplastic lymphoma kinase (ALK). J.Med.Chem. 61 4249 PMID:29660984 | |||
T37083 |
TL13-110
TL 13-110 |
Others | Others |
Negative control for TL 13-112 . Displays no degradation of ALK in cell lines. Highly potent ALK inhibitor (IC50 = 0.34 nM). Powell et al (2018) Chemically induced degradation of anaplastic lymphoma kinase. J.Med.Chem. 61 4249 PMID:29660984 | |||
T83856 |
AP-1
|
Others | Others |
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8152 |
6-Demethoxytangeretin
|
MAPK; ALK | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
6-Demethoxytangeretin 是一种从柑橘分离的黄酮。它能够促进 CRE 介导的转录 (与海马神经元的学习和记忆相关)。它具有抗炎和抗过敏作用,通过间变性淋巴瘤激酶和丝裂原活化蛋白激酶途径抑制人肥大细胞中 IL-6 的产生和基因表达。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPK-00927 |
ALK Protein, Mouse, Recombinant (hFc)
CD246,Anaplastic lymphoma kinase,... |
Mouse | HEK293 Cells |
Anaplastic lymphoma kinase (ALK) is mostly known for its oncogenic role in several human cancers. Recent evidences clearly indicate new roles of ALK and its genetic aberrations (e.g. gene rearrangements and mutations) in immune evasion, innate and cell-mediated immunity. New ALK-related immunotherapy approaches are demonstrating both preclinical and clinical promises. | |||
TMPY-02172 |
Midkine Protein, Human, Recombinant
midkine (neurite growth-promoting factor 2),NEGF2,MK,ARAP |
Human | Baculovirus Insect Cells |
Midkine (MK or MDK) also known as neurite growth-promoting factor 2 (NEGF2) is a basic heparin-binding growth factor of low molecular weight, and forms a family with pleiotrophin. Midkine is a retinoic acid-responsive, heparin-binding growth factor expressed in various cell types during embryogenesis. It promotes angiogenesis, cell growth, and cell migration. Midkine is also expressed in several carcinomas, suggesting that it may play a role in tumorigenesis, perhaps through its effects on angio... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10284 |
ALK-IN-6
|
Others | Others |
ALK-IN-6 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L). | |||
TMID-0073 |
Alectinib-d8
|
||
Alectinib-d8 是 Alectinib 的氘代化合物。Alectinib 的 CAS 号为 1256580-46-7。Alectinib 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。 |