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Catalog No.
ALK inhibitor,potent and ATP-competitive
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CH5424802 is a potent and selective ALK inhibitor.

Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers. .

In vitro: In cell free assays the IC50 of CH5424802 for enzyme activity of ALK was 1.9 nM; the dissociation constant (KD) value for ALK in an ATP-competitive manner was 2.4 nM. The inhibitory activity for two hot spot-activating mutations (F1174L and R1275Q) in neuroblastoma was comparable to that for wildtype ALK [1].

In vivo: In the NCI-H2228 model, oral administration of CH5424802 resulted in dose-dependent tumor growth inhibition (ED50 = 0.46 mg/kg) and tumor regression. Moreover, treatment of 20 mg/kg CH5424802 showed rapid tumor regression and tumor regrowth did not occur throughout the 4-week drug-free period [2].

Clinical trial: No clinical data are available currently.

[1] Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y.  CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.1256580-46-7
Solubilityinsoluble in H2O; ≥2.72 mg/mL in EtOH with gentle warming; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic
Chemical Name9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
SDFDownload SDF
Canonical SMILESCCC1=C(C=C2C(=C1)C(=O)C3=C(C2(C)C)NC4=C3C=CC(=C4)C#N)N5CCC(CC5)N6CCOCC6
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description Alectinib (CH5424802) is a potent inhibitor of ALK with an IC50 value of 1.9 nM.
Targets ALK (F1174L) ALK ALK (R1275Q) INSR KDR  
IC50 1 nM 1.9 nM 3.5 nM 550 nM 1.4 μM  

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Chemical structure