|
T6409 |
ALK kinase inhibitor-1
|
SAR348830 |
Others
|
|
SAR348830 is an ALK inhibitor, targeting anaplastic lymphoma kinase. |
|
T11254 |
F-1
|
|
ROS
,
ALK
,
ROS Kinase
|
|
F-1 is IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathwa... |
|
T3079 |
GSK1838705A
|
|
IGF-1R
,
JNK
,
S6 Kinase
,
ALK
|
|
GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases. |
|
T15612 |
JH-VIII-157-02
|
|
Microtubule Associated
,
ALK
|
|
JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L... |
|
T1962 |
ASP3026
|
ASP 3026 |
Apoptosis
,
ALK
|
|
ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS. |
|
T2612 |
CEP-28122
|
|
ALK
|
|
CEP-28122 is a highly potent and selective orally active ALK inhibitor. |
|
T16153 |
MS4078
|
|
ALK
,
Ligand for E3 Ligase
|
|
MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK. |
|
T3041 |
ALK inhibitor 2
|
|
FAK
,
ALK
|
|
ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase. |
|
T3059 |
ALK-IN-1
|
AP26113,Brigatinib,AP26113-analog |
EGFR
,
IGF-1R
,
ALK
|
|
ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2. |
|
T10285 |
ALK inhibitor 1
|
|
FAK
,
IGF-1R
,
ALK
|
|
ALK inhibitor 1 is a selective ALK kinase inhibitor. |
|
T4257 |
Belizatinib
|
TSR-011 |
Trk receptor
,
ALK
|
|
Belizatinib (TSR-011) is an effective, oral and dual inhibitor of ALK (IC50: 0.7 nM, wild-type recombinant ALK) and TRKA, TRKB, and TRKC. |
|
T1967 |
AZD-3463
|
ALK/IGF1R inhibitor |
Apoptosis
,
IGF-1R
,
ALK
,
Autophagy
|
|
AZD-3463 (ALK/IGF1R inhibitor) , an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency. |
|
T4015 |
HG-14-10-04
|
|
ALK
|
|
HG-14-10-04 is a potent and specific ALK inhibitor. |
|
T3621 |
Brigatinib
|
AP-26113 |
EGFR
,
FLT
,
ROS
,
IGF-1R
,
ALK
|
|
Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor. |
|
T4071 |
Repotrectinib
|
TPX-0005,TPX 0005,TPX0005 |
Trk receptor
,
ROS
,
Src
,
ALK
,
ROS Kinase
|
|
Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively. |
|
T1791 |
Ceritinib
|
LDK378 |
Serine Protease
,
IGF-1R
,
ALK
|
|
Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM). |
|
T1661 |
Crizotinib
|
PF-02341066 |
c-Met/HGFR
,
ROS
,
ALK
,
Autophagy
,
ROS Kinase
|
|
Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinases inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptor. |
|
T13416 |
ZX-29
|
|
ALK
|
|
ZX-29 is a potent and selective inhibitor of ALK(IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively), and also induces protective autophagy and has antitumor effect. |
|
T2655 |
CEP-37440
|
CEP37440 |
FAK
,
ALK
|
|
CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK). |
|
T3550 |
X-376
|
Ensartinib,X-396 |
c-Met/HGFR
,
ALK
|
|
X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inh... |
|
T2641 |
KRCA-0008
|
KRCA 0008,KRCA0008 |
ACK
,
ALK
|
|
KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability. |
|
T16708 |
R-268712
|
|
ALK
,
TGF-beta/Smad
|
|
R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor. |
|
T8399 |
Crizotinib hydrochloride
|
PF-02341066 hydrochloride |
c-Met/HGFR
,
ROS
,
ALK
,
Autophagy
,
ROS Kinase
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met(IC50s of 20 and 8 nM) |
|
T3678 |
Entrectinib
|
RXDX-101,NMS-E628 |
Trk receptor
,
ROS
,
ALK
,
Autophagy
,
ROS Kinase
|
|
Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectini... |
|
T3061 |
Lorlatinib
|
PF-6463922,PF-06463922,Loratinib |
Apoptosis
,
Tyrosine Kinases
,
ROS
,
ALK
,
ROS Kinase
|
|
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. |
|
T1791L |
Ceritinib dihydrochloride
|
LDK378 dihydrochloride |
IGF-1R
,
ALK
|
|
Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7... |
|
T22324 |
Ensartinib hydrochloride
|
Ensartinib dihydrochloride,X-396 dihydrochloride |
Others
,
Trk receptor
,
c-Met/HGFR
,
ALK
|
|
Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both... |
|
T1936 |
Alectinib
|
RG-7853,AF802,CH5424802,AF-802 |
VEGFR
,
Tyrosine Kinases
,
ALK
|
|
Alectinib (RG-7853) is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. |
|
T8387 |
Alectinib hydrochloride
|
CH5424802 (Hydrochloride),AF-802 (Hydrochloride),RO5424802 (Hydrochloride) |
ALK
|
|
Alectinib hydrochloride (RO5424802 Hydrochloride) is a selective, and orally available inhibitor of ALK( IC50 : 1.9 nM) |
|
T2251 |
NVP-TAE 684
|
TAE684 |
Apoptosis
,
ALK
|
|
NVP-TAE 684 (TAE684) is a excellently effective and specific ALK inhibitor(IC50=3 nM). |
|
T11184 |
EML4-ALK kinase inhibitor 1
|
EML4 ALK kinase inhibitor 1,EML4-ALK kinase inhibitor 1 |
ALK
|
|
EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM. |
|
T10284 |
ALK-IN-6
|
|
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). |
|
T10283 |
ALK-IN-5
|
|
ALK
|
|
ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK, IC50: 2.9 nM). |
|
T13781 |
MS4077
|
|
ALK
|
|
MS4077 is an degrader of anaplastic lymphoma kinase (ALK) PROTAC(Kd of 37 nM for binding affinity to ALK). |
|
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 patient... |
|
T73189 |
Ficonalkib
|
|
|
|
Ficonalkib is a potent antineoplastic agent that inhibits the Anaplastic Lymphoma Kinase (ALK) tyrosine kinase receptor. |
|
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 ... |
|
T72317 |
CEP-28122 mesylate salt
|
|
|
|
CEP-28122 mesylate salt, a diaminopyrimidine derivative, serves as a potent, selective, and orally bioavailable ALK (anaplastic lymphoma kinase) inhibitor, exhibiting an IC 50 value of 1.9 nM against recombinant ALK kina... |
|
T37083 |
TL13-110
|
TL 13-110 |
|
|
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. 6... |
|
T37084 |
TL13-22
|
TL 13-22 |
|
|
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.... |
|
T83856 |
AP-1
|
|
|
|
AP-1, a miniaturized proteolysis-targeting chimera (PROTAC) incorporating an anaplastic lymphoma kinase (ALK) ligand connected to (±)-thalidomide via an ultrashort linker, effectively degrades ALK fusion proteins such as... |
