CH5424802 (Synonyms: Alectinib, RO5424802) |
Catalog No.GC16025 |
CH5424802 (CH5424802) est un inhibiteur ALK puissant, sélectif et disponible par voie orale avec une IC50 de 1,9 nM et une valeur Kd de 2,4 nM (de manière compétitive avec l'ATP), et inhibe également ALK F1174L et ALK R1275Q avec des IC50 de 1 nM et 3,5 nM, respectivement. CH5424802 démontre une pénétration efficace du système nerveux central (SNC).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1256580-46-7
Sample solution is provided at 25 µL, 10mM.
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.
Reference:
[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.
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