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Cat.No. Product Name Information Product Use Citations Product Validations
S7998 Entrectinib (Rxdx-101) Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Verified customer review of Entrectinib (Rxdx-101)
S8901 Taletrectinib (DS-6051b) Taletretinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor, with ic50 values of 0.207 nM, 0.622 nM, 2.28 nM, and 0.980 nM for ROS1, NTRK1, NTRK2, and NTRK3, respectively.
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Sci Rep, 2024, 14(1):22191
Transl Lung Cancer Res, 2022, 11(11:2216-2229)
E1409 Zidesamtinib Zidesamtinib (NVL-520) is a potent brain-penetrating inhibitor of ROS1 tyrosine kinase with IC50 of 0.7 nM for wild-type ROS1 . It acts as a potential antineoplastic agent and can be used for the research of cancer.
S1068 PF-02341066 (Crizotinib) Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Signal Transduct Target Ther, 2025, 10(1):124
Cell Rep Med, 2025, S2666-3791(25)00102-8
Cell Death Differ, 2025, 10.1038/s41418-025-01510-x
Verified customer review of PF-02341066 (Crizotinib)
S7536 Lorlatinib (PF-6463922) Lorlatinib (PF-6463922) 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. PF-06463922 induces apoptosis. Phase 1.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Death Dis, 2025, 16(1):194
Mol Oncol, 2025, 19(2):519-539
Verified customer review of Lorlatinib (PF-6463922)
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Nat Commun, 2023, 14(1):2829
Cancer Res Commun, 2023, 3(4):659-671
S8229 Brigatinib Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Death Dis, 2025, 16(1):194
Toxicol Appl Pharmacol, 2025, 498:117310
Verified customer review of Brigatinib
S8583 Repotrectinib (TPX-0005) Repotrectinib (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); it is also a potent SRC inhibitor (IC50 5.3 nM).
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Commun Biol, 2024, 7(1):412
Cancer Discov, 2023, 13(3):598-615
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. This compound also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
Mol Oncol, 2025, 19(8):2366-2387
NPJ Breast Cancer, 2024, 10(1):65
Cancers (Basel), 2024, 16(12)2253