CJ-2360 

CJ-2360 is a potent and orally active ALK inhibitor with IC₅₀s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated^[1].

CJ-2360 achieves an IC₅₀ value of 1.8 nM in inhibition of cell growth in the KARPAS-299 cell line. Further tested CJ-2360 for its potency in cell growth inhibition in the H3122 non-small-cell lung cell line carrying EML4-ALK and obtained an IC₅₀ value of 3 nM. CJ-2360 inhibits Mer tyrosine-protein kinase (MERTK), CLK1, DAPK1, DAPK2, and DAPK3 with IC₅₀s of 6.3, 11, 31, 23, 22, and 260 nM, respectively. CJ-2360 displays >100-fold selectivity for ALK over the insulin receptor kinase (INSR) and shows no significant activity against IGF1R^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CJ-2360 (100 mg/kg; p.o.; twice daily for 22 days) is capable of achieving complete and long-lasting tumor regression in the KARPAS-299 xenograft tumor model^[1].
CJ-2360 (100 mg/kg; p.o.) is very effective in inhibition of ALK phosphorylation, as well as ERK and STAT3 phosphorylation in KARPAS-299 tumor tissue, with the effect persisting for at least 24 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

475.56

C₂₇H₃₀FN₅O₂

2226742-61-4

N#CC1=CC(N2)=C(C3=C2N(C(C)C)C4=C(C=C(OC)C(N5C[C@H](C)N(C)[C@H](C)C5)=C4F)C3=O)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Chen J, et al. Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. J Med Chem. 2020;63(22):13994-14016.  [Content Brief]