ALK

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
S8700 TP0427736 HCl <1 mg/mL 67 mg/mL <1 mg/mL
S5232 Alectinib hydrochloride <1 mg/mL 2 mg/mL <1 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
S8583 TPX-0005 <1 mg/mL 70 mg/mL 10 mg/mL
S8229 Brigatinib (AP26113) <1 mg/mL 1 mg/mL 43 mg/mL
S8511 Belizatinib (TSR-011) <1 mg/mL 100 mg/mL 100 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
S8230 Ensartinib (X-396) <1 mg/mL 100 mg/mL 100 mg/mL
Catalog No. Information Product Use Citations Product Validations
S1068

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.

S1108

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.

S2762

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.

S7083

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.

S7000

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.

S8700New

TP0427736 HCl

TP0427736 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.

S5232New

Alectinib hydrochloride

Alectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.

S2703

GSK1838705A

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.

S7106

AZD3463

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

S8054

ASP3026

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

S7998

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.

S8583

TPX-0005

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).

S8229

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.

S8511

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). "

S7148

ML347

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.

S7536

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.

S8230

Ensartinib (X-396)

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

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