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Alectinib (CH5424802) is a highly selective, orally active and potent ALK inhibitor with IC50 of 1.9 nM. Alectinib (CH5424802) also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration. Alectinib (CH5424802) 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. Alectinib (CH5424802) inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors. Alectinib (CH5424802) also blocked EML4-ALK L1196M-driven cell growth.
Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression in SCID or nude mice bearing NCI-H2228 cells.
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Source | Cancer Cell (2011). Figure 5. CH5424802 |
| Method | Cell Viability Assay | |
| Cell Lines | NSCLC Cell Lines | |
| Concentrations | 0~1000 nM | |
| Incubation Time | 5 days | |
| Results | CH5424802 was preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCIH522 cells (EGFR wild-type, KRAS wild-type, and ALK wildtype) in monolayer culture |
| 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 (M4839) or CellTiter-Glo luminescent cell viability assay. Caspase-3/7 assay was evaluated using the Caspase-Glo 3/7 Assay Kit. |
| 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 |
| Molecular Weight | 482.62 |
| Formula | C30H34N4O2 |
| CAS Number | 1256580-46-7 |
| Solubility (25°C) | DMSO 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| AP26113 (Brigatinib)
AP26113 (Brigatinib) is a highly potent ALK inhibitor with IC50 of 0.6 nM. |
| X-376
X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitor with IC50 of 0.61 nM. |
| SB431542
SB-431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM). |
| RepSox
RepSox (ALK5 Inhibitor II) is a potent and ATP-competitive inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively). |
| LDN-193189
LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
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