ALK

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ALK Inhibitors (10)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Nature, 2012, 487(7408):505-9
  • Cell, 2012, 151(5):937-50
  • Nat Med, 2012, 18(6):883-91
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.
  • Nature, 2012, 487(7408):505-9
  • Cell, 2012, 151(5):937-50
  • Cancer Cell, 2015, 27(3):397-408
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.
  • Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913
  • Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0016
  • Oncotarget, 2014, 5(13):4920-8
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.
  • Cancer Cell, 2015, 27(3):397-408
  • Cell Res, 2015, 10.1038/cr.2015.16
  • Mol Oncol, 2015, 10.1016/j.molonc.2015.11.007
S7000 AP26113 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.
  • Clin Cancer Res, 2015, 21(1):166-74
  • Clin Cancer Res, 2014, 20(22):5686-96
  • Jpn J Clin Oncol, 2014, 44(10):963-8
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.
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.
  • Cancer Res, 2014, 74(24):7217-28
  • Mol Cell Proteomics, 2012, 11(6):M112.017764
  • Cancer Chemoth Pharm, 2015, 10.1007/s00280-015-2751-6
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency.
  • PLoS One, 2015, 10(11):e0142704
S7536 PF-06463922 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.
S8054 ASP3026 ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
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 <1 mg/mL 45 mg/mL 106 mg/mL
S7998 Entrectinib (RXDX-101) <1 mg/mL 100 mg/mL 100 mg/mL
S2703 GSK1838705A <1 mg/mL 107 mg/mL <1 mg/mL
S7106 AZD3463 <1 mg/mL 24 mg/mL <1 mg/mL
S7536 PF-06463922 <1 mg/mL 81 mg/mL 30 mg/mL
S8054 ASP3026 <1 mg/mL 14 mg/mL <1 mg/mL
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