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CH5424802

Cat. No. M1942
CH5424802 Structure
Synonym:

AF802

Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 280 In stock
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Quality Control
Biological Activity

CH5424802 (AF802) is a potent, selective, and orally available ALK inhibitor. Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered an attractive therapeutic target for human cancers. CH5424802 (AF802) showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors. CH5424802 also blocked EML4-ALK L1196M-driven cell growth.

Protocol
Cell Experiment
Cell lines KARPAS-299, SR, HDLM-2, NB-1, NCI-H2228, MKN-45, SK-BR-3 cells
Preparation method Cell growth inhibition and caspase-3/7 assay
Cells were incubated with various concentrations of compound for the indicated time. The viable cells were measured by Cell Counting Kit-8 assay (Dojindo Laboratories) or CellTiter-Glo luminescent cell viability assay (Promega). Caspase-3/7 assay was evaluated using the Caspase-Glo 3/7 Assay Kit (Promega).
Concentrations 0~10 μM
Incubation time 96 h
Animal Experiment
Animal models SCID mice
Formulation water
Dosages 6, 20 and 60mg/kg for 7 days
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 482.62
Formula C30H34N4O2
CAS Number 1256580-46-7
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
Kinoshita K, et al. Bioorg Med Chem. 2012 Feb 1;20(3):1271-80. PMID: 22225917.

CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.
Sakamoto H, et al. Cancer Cell. 2011 May 17;19(5):679-90. PMID: 21575866.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CH5424802, AF802 supplier, ALK, inhibitors

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