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| Catalog No. | Inhibitor Name | ALK | Other |
|---|---|---|---|
| A10712 | Crizotinib | * | c-Met |
| A10662 | TAE684 | ** | |
| A11134 | Alectinib | ** | INSR,KDR |
| A13238 | Ceritinib | **** | Insulin Receptor,IGF-1R,STK22D |
| A11948 | AP26113 | *** | FER,ROS/ROS1,FLT3 |
| A11175 | GSK1838705A | *** | Insulin Receptor,IGF-1R,RSK1 |
| A13065 | AZD3463 | *** | |
| A11773 | ASP3026 | * | |
| A14207 | PF-06463922 | **** | LTK (TYK1),FER,FES (FPS) |
| A15801 | Entrectinib | TrkC,TrkB,TrkA | |
| A13450 | Brigatinib (AP26113) | **** | FLT3,IGF1R,EGFR(C797S/del19) |
| A13744 | CEP-28122 | **** | |
| A15511 | KRCA-0008 | *** | Ack1 |
| A15543 | CEP-37440 | ** | FAK |
| A16267 | HG-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.
45 Item(s)
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Ensartinib hydrochloride
Catalog No. A21719 ALK/MET inhibitorEnsartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. Learn More -
Entrectinib
Catalog No. A15801 TRK, ROS1, ALK inhibitorEntrectinib, 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. Learn More -
Brigatinib (AP26113)
Catalog No. A13450 ALK InhibitorBrigatinib (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. Learn More -
LDN-214117
Catalog No. A16096 ALK2 inhibitorLDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. Learn More -
R-268712
Catalog No. A16207 ALK5 inhibitorR-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM. Learn More -
Crizotinib hydrochloride
Catalog No. A16245 c-Met/NPM-ALK inhibitorCrizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Learn More -
HG-14-10-04
Catalog No. A16267 ALK inhibitorHG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM. Learn More -
WY-135
Catalog No. A20071 ALK/ ROS1 dual inhibitorWY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor. Learn More -
ALK2-IN-2
Catalog No. A13604 Alk2 inhibitorALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3. Learn More -
Alectinib Hydrochloride
Catalog No. A18000 ALK inhibitorAlectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Learn More -
Belizatinib
Catalog No. A20919 ALK/TRKA/TRKB/TRKC inhibitorBelizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7?nM for wild-type recombinant ALK kinase. Learn More -
KRCA-0008
Catalog No. A15511 ACK1/ALK inhibitorKRCA-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. Learn More -
X-376
Catalog No. A20971 ALK inhibitorX-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity. Learn More -
F-1
Catalog No. A19269 ALK and ROS1 dual inhibitorF-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. Learn More -
Ensartinib
Catalog No. A19720 ALK/MET inhibitorEnsartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. Learn More -
SM 16
Catalog No. A19765 ALK5/ALK4 inhibitorSM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively. Learn More -
MS4077
Catalog No. A20077 ALK PROTAC degraderMS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37?nM for binding affinity to ALK. Learn More -
MS4078
Catalog No. A20089 ALK PROTAC degraderMS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19?nM for binding affinity to ALK. Learn More -
JH-VIII-157-02
Catalog No. A20205 ALK inhibitorJH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. Learn More -
TP0427736 HCl
Catalog No. A22382 ALK5 kinase activity inhibitorTP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. Learn More -
BIO-013077-01
Catalog No. A22185 antagonist of the TGFbeta family type I receptors, Alk5 and/or Alk4BIO-013077-01, Novel potent antagonist of the TGFbeta family type I receptors, Alk5 and/or Alk4. Learn More -
ALK2-IN-1
Catalog No. A22183 inhibitor of Activin receptor-like kinase (ALK2) mutant R206HALK2-IN-1 (BLU-782) is a potent and selective inhibitor of Activin receptor-like kinase (ALK2) mutant R206H with binding IC50 of <10 nM. Learn More -
AZD3463
Catalog No. A13065 -
TAE684
Catalog No. A10662 ALK InhibitorTAE684 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). Learn More -
SB-505124
Catalog No. A11157 ALK5 inhibitorSB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). Learn More -
GSK1838705A
Catalog No. A11175 IGF-1R InhibitorGSK1838705A 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.
Learn More -
LDN193189
Catalog No. A11205 ALK inhibitorLDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation. Learn More -
SB 525334
Catalog No. A10827 ALK InhibitorSB525334 is a selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells Learn More -
CH5424802
Catalog No. A11134 ALK InhibitorCH5424802 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. Learn More -
ASP3026
Catalog No. A11773 ALK inhibitorASP3026 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. Learn More -
ALK-IN-1 (Brigatinib analog, AP26113 analog)
Catalog No. A11948 ALK inhibitorAP26113 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] Learn More -
A 83-01
Catalog No. A12358 TGF-β/ALK5 inhibitorA83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7 Learn More -
DMH-1
Catalog No. A12820 ALK2 inhibitorDMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM). Learn More -
LDK-378
Catalog No. A13238 ALK InhibitorLDK378 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. Learn More -
PF-2341066 (Crizotinib)
Catalog No. A10712 ALK/ c-Met inhibitorPF-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). Learn More -
CEP-28122
Catalog No. A13744 ALK inhibitorCEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers. Learn More -
EW-7197 (Vactosertib)
Catalog No. A14213 ALK4/ALK5 inhibitorEW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively Learn More -
PF-06463922
Catalog No. A14207 ALK inhibitorPF-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. Learn More -
WZ4003
Catalog No. A14312 NUAK kinase inhibitorWZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2 Learn More -
A 77-01
Catalog No. A14436 ALK5 inhibitorA 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. Learn More -
LDK378 (Ceritinib) dihydrochloride
Catalog No. A15142 ALK inhibitorLDK378 dihydrochloride is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Learn More -
ALK inhibitor 1
Catalog No. A14987 ALK inhibitorALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase. Learn More -
ALK inhibitor 2
Catalog No. A14988 ALK inhibitorALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase. Learn More -
CEP-37440
Catalog No. A15543 FAK/ALK inhibitorCEP-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). Learn More -
ALK-IN-6
Catalog No. A18457 ALK inhibitorALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively. Learn More
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