Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1068 Crizotinib (PF-02341066) <1 mg/mL 9 mg/mL <1 mg/mL
S1108 TAE684 (NVP-TAE684) <1 mg/mL 3 mg/mL <1 mg/mL
S2762 Alectinib (CH5424802) <1 mg/mL 0.5 mg/mL <1 mg/mL
S7083 Ceritinib (LDK378) <1 mg/mL 20 mg/mL 3 mg/mL
S7000 AP26113-analog (ALK-IN-1) <1 mg/mL 45 mg/mL 106 mg/mL
S8230 Ensartinib (X-396) <1 mg/mL 100 mg/mL 100 mg/mL
S8511 Belizatinib (TSR-011) <1 mg/mL 100 mg/mL 100 mg/mL
S8583 TPX-0005 <1 mg/mL 70 mg/mL 10 mg/mL
S8229 Brigatinib (AP26113) <1 mg/mL 1 mg/mL 43 mg/mL
S2703 GSK1838705A <1 mg/mL 107 mg/mL <1 mg/mL
S7106 AZD3463 <1 mg/mL 24 mg/mL <1 mg/mL
S8054 ASP3026 <1 mg/mL 14 mg/mL <1 mg/mL
S7998 Entrectinib (RXDX-101) <1 mg/mL 100 mg/mL 75 mg/mL
S7148 ML347 <1 mg/mL 10 mg/mL <1 mg/mL
S7536 Lorlatinib (PF-6463922) <1 mg/mL 81 mg/mL 30 mg/mL
Catalog No. Information Product Use Citations Product Validations

Crizotinib (PF-02341066)

Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively.


TAE684 (NVP-TAE684)

TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR.


Alectinib (CH5424802)

Alectinib (CH5424802) is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.


Ceritinib (LDK378)

Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.


AP26113-analog (ALK-IN-1)

AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.


Ensartinib (X-396)

Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays.


Belizatinib (TSR-011)

"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "



TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).


Brigatinib (AP26113)

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.



GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.



AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency.



ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.


Entrectinib (RXDX-101)

Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.



ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.


Lorlatinib (PF-6463922)

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. Phase 1.

Tags: ALK inhibition | ALK cancer | ALK mutation | ALK tumor | ALK inhibitor drugs | ALK activation | ALK targets | ALK inhibitor cancer | ALK assay | ALK phosphorylation | ALK signaling pathway | ALK inhibitor clinical trial | ALK inhibitor review