1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. CJ-2360

CJ-2360 

Cat. No.: HY-131909
Handling Instructions

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.

For research use only. We do not sell to patients.

CJ-2360 Chemical Structure

CJ-2360 Chemical Structure

CAS No. : 2226742-61-4

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Description

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].

In Vitro

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].

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

In Vivo

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].

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

Animal Model: KARPAS-299 xenograft model (female SCID mice)[1]
Dosage: 100 mg/kg
Administration: P.o.; twice daily for 22 days
Result: Very efficacious in the KARPAS-299 xenograft model. It achieves complete tumor regression in 100% of tumors and all tumors did not return until day 53, 23 days after the last dose.
Molecular Weight

475.56

Formula

C₂₇H₃₀FN₅O₂

CAS No.

2226742-61-4

SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

CJ-2360CJ2360CJ 2360ALKAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246oraltumorregressionKARPAS-299xenograftmodelmutantsInhibitorinhibitorinhibit

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CJ-2360
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HY-131909
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