ALK

Inhibitory Selectivity
Catalog No.Inhibitor Name ALKOther
A10712Crizotinib
*
c-Met
A10662TAE684
**
A11134Alectinib
**
INSR,KDR
A13238Ceritinib
****
Insulin Receptor,IGF-1R,STK22D
A11948AP26113
***
FER,ROS/ROS1,FLT3
A11175GSK1838705A
***
Insulin Receptor,IGF-1R,RSK1
A13065AZD3463
***
A11773ASP3026
*
A14207PF-06463922
****
LTK (TYK1),FER,FES (FPS)
A15801Entrectinib
TrkC,TrkB,TrkA
A13450Brigatinib (AP26113)
****
FLT3,IGF1R,EGFR(C797S/del19)
A13744CEP-28122
****
A15511KRCA-0008
***
Ack1
A15543CEP-37440
**
FAK
A16267HG-14-10-04
***

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



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Catalog No. Product Name Application Product Information
A16267

HG-14-10-04

ALK inhibitor
HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
A16245

Crizotinib hydrochloride

c-Met/NPM-ALK inhibitor
Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.
A15801

Entrectinib

TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.
A15511

KRCA-0008

ACK1/ALK inhibitor
KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.
A15543

CEP-37440

FAK/ALK inhibitor
CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).
A15142

LDK378 dihydrochloride

ALK inhibitor
LDK378 dihydrochloride is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
A14207

PF-06463922

ALK inhibitor
PF-06463922 is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.
A13065

AZD3463

ALK/IGF1R inhibitor
AZD-3463 is a ALK/IGF1R inhibitor.
A10662 SALE

TAE684

ALK Inhibitor
TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).
A13450

Brigatinib (AP26113)

ALK Inhibitor
Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
A11175 SALE

GSK1838705A

IGF-1R Inhibitor

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.

A11134 SALE

CH5424802

ALK Inhibitor
CH5424802 is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK.
A11773

ASP3026

ALK inhibitor
ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel.
A14988

ALK inhibitor 2

ALK inhibitor
ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
A14987

ALK inhibitor 1

ALK inhibitor
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
A11948 SALE

AP26113 (Brigatinib)

ALK inhibitor
AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. [1][2] AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. [3]
A13238 SALE

LDK-378

ALK Inhibitor
LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target.
A13744

CEP-28122

ALK inhibitor
CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
A10712 SALE

PF-2341066 (Crizotinib)

ALK/ c-Met inhibitor
PF-2341066 (Crizotinib) is an inhibitor of the c-Met kinase and the NPM-ALK. PF-2341066 inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).

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