crizotinib

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

(S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

2-Keto Crizotinib is an active lactam metabolite of crizotinib.

Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met, with IC50 values of 20 nM and 8 nM, respectively.

Crizotinib-d5 is a deuterated compound of Crizotinib. Crizotinib has a CAS number of 877399-52-5. Crizotinib is an ATP-competitive small-molecule tyrosine kinases inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptor.

Crizotinib, an orally bioavailable agent, belongs to the class of c-met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors with potential antineoplastic activity.

IR-Crizotinib is a conjugate of the near-infrared dye IR-786 and Crizotinib, an NF-κB-inducing kinase (NIK) inhibitor, with an IC50 of 3.381 μM for intracranial glioblastoma (GBM) localization in mice. It has the ability to cross the blood-brain barrier and fluorescently mark GBM, and demonstrates efficacy in inhibiting glioma proliferation and invasion both in vitro and in vivo, making it significant in cancer research [1].

ALK-IN-1 (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.

ALK/ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK/ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme).

KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.

Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.

Poloppin is a protein-protein interactions modulator of the mitotic polo-like kinases that acts by targeting mutant KRAS. It works synergistically with Crizotinib, an inhibitor of the c-MET receptor, against mutant KRAS-expressing cancer cells.

PRO-6E is an orally active, Cereblon ligand-based PROTAC that promotes MET degradation, achieving up to 81.9% effectiveness at a concentration of 1 μM in MKN-45 cells. It demonstrates tumor growth inhibition both in vivo and in vitro, alongside inducing cell apoptosis and cell cycle arrest. Notably, its structure comprises a Cereblon ligand (blue), a linker (black), and an ALK/c-Met inhibitor Crizotinib component (pink). [1]

Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1 NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations.

Taletrectinib (AB-106) is a new-generation selective inhibitor of ROS1/NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.

X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins, and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development.

PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).

AZD-3463 (ALK IGF1R inhibitor), an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.