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Alectinib (formerly AF802, CH5424802, RO5424802; trade name Alecensa) is a potent, selective, and orally bioavailable ALK (anaplastic lymphoma kinase) tyrosine kinase inhibitor with potential antitumor activity. In cell-free assays, it inhibits ALK with an IC50 value of 1.9 nM. The Food and Drug Administration (FDA) authorized alelectinib in 2017 for the management of patients with non-small cell lung cancer (NSCLC) that was positive for ALK.
| Targets |
ALK (IC50 = 1.9 nM); ALKF1174L (IC50 = 1 nM); ALKR1275Q (IC50 = 3.5 nM); ALK (Kd = 2.4 nM)
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| ln Vitro |
Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment was able to prevent autophosphorylation of ALK and significantly suppress phosphorylation of STAT3 and AKT, in NCI-H2228 cells expressing EML4-ALK[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[1]. |
| ln Vivo |
Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells), tumor regression and dose-dependent inhibition of tumor growth (EC50 of 0.46 mg/kg) are possible outcomes of treatment. There are no noticeable toxicity symptoms or variations in body weight at any dosage level[1].
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| Enzyme Assay |
Through the use of time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay, the inhibitory ability against each kinase—apart from MEK1 and Raf-1—is assessed by looking at their capacity to phosphorylate different substrate peptides in the presence of CH542480. The phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802 is quantitatively analyzed to determine the inhibitory activity against MEK1. When CH5424802 is present, the kinases' capacity to phosphorylate MEK1 is used to gauge their inhibitory activity against Raf-1.
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| Cell Assay |
In 96-well plates, cells such as NSCLC, A549, and HCC827 are seeded overnight and then incubated with different concentrations of CH5424802 for the specified amount of time. In the spheroid cell growth inhibition assay, the compound is added to cells that have been seeded on spheroid plates, incubated for a full night, and then treated for the designated durations. The Luminescent Cell Viability Assay is used to determine the number of viable cells. The Caspase-Glo 3/7 Assay Kit is used to evaluate the Caspase-3/7 assay.
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| Animal Protocol |
SCID or nude mice bearing NCI-H2228
20 mg/kg Oral administration |
| References |
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| Molecular Formula |
C30H34N4O2
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|---|---|
| Molecular Weight |
482.62
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| Exact Mass |
482.27
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| Elemental Analysis |
C, 74.66; H, 7.10; N, 11.61; O, 6.63
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| CAS # |
1256580-46-7
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| Related CAS # |
Alectinib Hydrochloride;1256589-74-8;Alectinib-d8;1256585-15-5;Alectinib-d6;1616374-19-6
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| Appearance |
White to off-white solidw powder
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| SMILES |
CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C
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| InChi Key |
KDGFLJKFZUIJMX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3
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| Chemical Name |
9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
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| Synonyms |
Alectinib; CH5424802; CH 5424802; RO 5424802; AF802; CH-5424802; RO5424802; AF 802; AF-802; RO-5424802; brand name: Alecensa
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0720 mL | 10.3601 mL | 20.7202 mL | |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0720 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02075840 | Active Recruiting |
Drug: Alectinib Drug: Crizotinib |
Non-Small Cell Lung Cancer | Hoffmann-La Roche | August 19, 2014 | Phase 3 |
| NCT03596866 | Active Recruiting |
Drug: Brigatinib Drug: Alectinib |
ALK+ Advanced NSCLC | Takeda | April 19, 2019 | Phase 3 |
| NCT03202940 | Recruiting | Drug: Alectinib Drug: Cobimetinib |
Non-small Cell Lung Cancer | Massachusetts General Hospital | September 14, 2017 | Phase 1 Phase 2 |
| NCT05770037 | Recruiting | Drug: Alectinib | Solid Tumor Cancer |
Cancer Research UK | August 17, 2022 | Phase 2 Phase 3 |
| NCT05525338 | Recruiting | Drug: Alectinib | Drug Monitoring Lung Cancer |
University Medical Center Groningen |
March 23, 2022 | Phase 4 |
The structure and cytotoxicity of alectinib.Exp Mol Med. 2017 Mar; 49(3): e303. |
Potentiation of the anticancer effects of paclitaxel by alectinib in the KBv200 cell xenograft nude mice model. The tumor growth curve was drawn to monitor the tumor volume with time after implantation. The data shown are expressed as the mean±s.d. of the tumor volume for each group (n=9) (a).Exp Mol Med. 2017 Mar; 49(3): e303. |
Effect of alectinib on the intracellular accumulations of DOX and Rho 123 in MDR cells and in their parental sensitive cells.Exp Mol Med. 2017 Mar; 49(3): e303. |
Effect of alectinib on the efflux of Rho 123, ATPase activity and the [125I]-IAAP photoaffinity labeling of ABCB1 and ABCG2.Exp Mol Med. 2017 Mar; 49(3): e303. |
Effect of alectinib on the expression levels of ABCB1 or ABCG2 in MDR cells.Exp Mol Med. 2017 Mar; 49(3): e303. |
Effect of alectinib on the inhibition of AKT, ERK and c-Met phosphorylation.Exp Mol Med. 2017 Mar; 49(3): e303. |
Alectinib increased the accumulation of Rho 123 and enhanced the cytotoxicity of DOX in ABCB1-overexpressing primary leukemia blasts.Exp Mol Med. 2017 Mar; 49(3): e303. |
A schematic model illustrating the reversal of MDR by alectinib.Exp Mol Med. 2017 Mar; 49(3): e303. |
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