Model No.: CAS 1256580-46-7
Productivity: 1 kg/month
Place of Origin: China
Supply Ability: 1 kg
Certificate: ISO 9001, gmp
Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, 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, and blocked EML4-ALK L1196M-driven cell growth.
|Storage temp||Store at RT|
|Appearance||White to Off-White Solid|
|Usage||treatment of patients with ALK-driven tumors.|
Alectinib (CH5424802) is an ATP-competitive inhibitor for ALK and L1196M with Ki values of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK, and also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 elicits an apoptotic marker—caspase-3/7-like activation—in NCI-H2228 spheroid cells. CH5424802 blocks the growth of two NPM-ALK expressing lymphoma lines, KARPAS-299 and SR with greater efficacy against KARPAS-299 at an IC50 of 3 nM.
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