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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 |
|---|
| F-1
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
| TL13-22
TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. |
| TL13-110
TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. |
| ALK inhibitor 2
ALK inhibitor 2 is a potent pyrimidin ALK inhibitor. |
| NVL-655 TFA
NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
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