Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and 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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 91 | |
4 mg | In stock | $ 172 | |
8 mg | In stock | $ 260 | |
20 mg | In stock | $ 451 | |
40 mg | In stock | $ 712 |
Description | Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and 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. |
Targets&IC50 | ALK: 1.9 nM, ALK (R1275Q): 3.5 nM, ALK (F1174L): 1 nM |
In vitro | Cells including NSCLC, A549 and HCC827 are seeded in 96-well plates overnight and incubated with various concentrations of CH5424802 for the indicated time. For spheroid cell growth inhibition assay, cells are seeded on spheroid plates, incubated overnight, and then treated with compound for the indicated times. The viable cells are measured by the Luminescent Cell Viability Assay. Caspase-3/7 assay is evaluated using the Caspase-Glo 3/7 Assay Kit.(Only for Reference) |
Synonyms | CH5424802, RG-7853, AF-802, AF802 |
CAS No. | 1256580-46-7 |
Chemical Formula | C30H34N4O2 |
Molecular Weight | 482.628 |
Solubility | H2O: 2.1 mM DMSO: 12.4 mM |
Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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