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Cat. No.: HY-131909

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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.

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CAS No.: 2226742-61-4
Formule: C₂₇H₃₀FN₅O₂
Masse moléculaire:475.56

Stockage:

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

Data Sheet (271 KB)

CJ-2360 Chemical Structure

CAS No.: 2226742-61-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
KARPAS-299	IC₅₀	1.8 nM Compound: CJ-2360	Antiproliferative activity against human KARPAS-299 cells incubated for 4 days by WST8 or Cell-titer-Glo assay Antiproliferative activity against human KARPAS-299 cells incubated for 4 days by WST8 or Cell-titer-Glo assay	[PMID: 33185101]
NCI-H3122	IC₅₀	3 nM Compound: CJ-2360	Antiproliferative activity against human NCI-H3122 cells incubated for 4 days by WST8 or Cell-titer-Glo assay Antiproliferative activity against human NCI-H3122 cells incubated for 4 days by WST8 or Cell-titer-Glo assay	[PMID: 33185101]

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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS No. 2226742-61-4
Masse moléculaire 475.56
Formule C₂₇H₃₀FN₅O₂
SMILES

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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