| Identification | Back Directory | [Name]
5H-Quinindoline-8-carbonitrile, 4-fluoro-6,11-dihydro-2-methoxy-5-(1-methylethyl)-11-oxo-3-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- | [CAS]
2226742-61-4 | [Synonyms]
CJ-2360
5H-Quinindoline-8-carbonitrile, 4-fluoro-6,11-dihydro-2-methoxy-5-(1-methylethyl)-11-oxo-3-[(3R,5S)-3,4,5-trimethyl-1-piperazinyl]-, rel- | [Molecular Formula]
C27H30FN5O2 | [MDL Number]
MFCD33023477 | [MOL File]
2226742-61-4.mol | [Molecular Weight]
475.57 |
| Hazard Information | Back Directory | [Uses]
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 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]. | 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.
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| [References]
[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. DOI:10.1021/acs.jmedchem.0c01550 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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