Alectinib Hydrochloride
Based on 44 publication(s) in Google Scholar
Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.92%
- CAS. Nr.: 1256589-74-8
- Formel: C30H35ClN4O2
- Molecular Weight:519.08
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-12857
BrigatinibALK Inhibitor -
HY-12215
LorlatinibALK/ROS1 Inhibitor -
HY-13011
AlectinibALK Inhibitor -
HY-13011AR
Alectinib Hydrochloride (Standard)ALK Inhibitor -
HY-50878A
Crizotinib hydrochlorideALK/c-Met Inhibitor -
HY-50878
CrizotinibALK/c-Met/ROS1 Inhibitor -
HY-103022
RepotrectinibROS1/TRK/ALK Inhibitor -
HY-15656A
Ceritinib dihydrochlorideALK Inhibitor -
HY-103714A
Ensartinib dihydrochlorideALK/MET Inhibitor -
HY-12215R
Lorlatinib (Standard)ALK/ROS1 Inhibitor -
HY-14660
DabrafenibBRAF Inhibitor -
HY-10181
DasatinibSrc/Bcr-Abl Inhibitor
Publications Citing Use of MedChemExpress (MCE) Alectinib Hydrochloride
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Science. 2014 Oct 3;346(6205):1255784. [Abstract]
- Cell. 2025 Mar 6;188(5):1248-1264.e23. [Abstract]
- Cancer Discov. 2026 Jun 22. [Abstract]
- Cancer Discov. 2024 Dec 2;14(12):2367-2386. [Abstract]
- Cancer Discov. 2018 Jun;8(6):714-729. [Abstract]
- Cancer Discov. 2016 Oct;6(10):1118-1133. [Abstract]
- Nat Cancer. 2022 Jun;3(6):710-722. [Abstract]
- Cancer Res. 2022 Feb 1;82(3):484-496. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2022 Oct 3;13(1):5745. [Abstract]
- Cell Discov. 2021 May 11;7(1):33. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]
- Cell Death Discov. 2018 May 10:4:56. [Abstract]
- Oncogene. 2022 Sep;41(40):4547-4559. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- Aging Cell. 2020 May;19(5):e13137. [Abstract]
- Sci Signal. 2022 Oct 25;15(757):eabm0808. [Abstract]
- Pharmaceutics. 2023 Oct 11;15(10):2449. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Biomolecules. 2024 May 28;14(6):631. [Abstract]
- Microchem J. 2025 Nov 3;219:116046.
- BMC Chem. 2025 Aug 22;19(1):248. [Abstract]
- Cancer Sci. 2025 Jul 23. [Abstract]
- Transl Oncol. 2021 Jan;14(1):100887. [Abstract]
- Neoplasia. 2023 Aug:42:100908. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- PLoS One. 2025 Jan 21;20(1):e0308747. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Cell Physiol Biochem. 2018;51(5):1996-2009. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Biol Pharm Bull. 2026;49(1):122-129. [Abstract]
- Biomed Chromatogr. 2024 Oct;38(10):e5986. [Abstract]
- bioRxiv. 2025 Dec 5.
- Patent. US20250003968A1.
- Research Square Preprint. 2024 Nov 26.
- Heliyon. 2024 Sep 28;10(19):e38637. [Abstract]
- University of California. 2024.
- bioRxiv. 2021 Nov 12.
- bioRxiv. 2020 Dec 16:2020.08.14.251207. [Abstract]
Customer Validation & Images
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Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 1.9 nM (ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]
In Vitro
Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:NCI-H2228 cells
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Concentration:0 nM,10 nM,100 nM, 1000 nM
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Incubation Time:2 hours
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Result:Inhibition of ALK phosphorylation and signal transduction.
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Cell Line:HCC827, A549, or NCIH522 cells
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Concentration:0-1000 nM
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Incubation Time:5 days
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Result:Reduced cell activity in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID or nude mice bearing NCI-H2228 cells[1]
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Dosage:0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
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Administration:Oral administration; once daily; for 11 days
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Result:Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.
Chemical Information
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CAS. Nr. 1256589-74-8
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Appearance Solid
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Molecular Weight 519.08
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Formel C30H35ClN4O2
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Color White to off-white
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SMILES
[H]Cl.N#CC1=CC2=C(C3=C(N2)C(C)(C4=CC(N5CCC(CC5)N6CCOCC6)=C(C=C4C3=O)CC)C)C=C1
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Synonyms
CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (44)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Science
2014 Oct 3;346(6205):1255784. PMID: 25278616 -
Cell
2025 Mar 6;188(5):1248-1264.e23. PMID: 39919745 -
Cancer Discov
EML4-ALK mediates resistance to KRAS G12C inhibition and induces an oncogenic dependency by rewiring signaling through the wild-type RAS pathway. [Abstract]2026 Jun 22. PMID: 42329099 -
Cancer Discov
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]2024 Dec 2;14(12):2367-2386. PMID: 39269178 -
Cancer Discov
Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer. [Abstract]2018 Jun;8(6):714-729. PMID: 29650534 -
Cancer Discov
Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer. [Abstract]2016 Oct;6(10):1118-1133. PMID: 27432227 -
Nat Cancer
Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer. [Abstract]2022 Jun;3(6):710-722. PMID: 35726063 -
Cancer Res
2022 Feb 1;82(3):484-496. PMID: 34853072 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2022 Oct 3;13(1):5745. PMID: 36192379 -
Cell Discov
Phase separation of EML4-ALK in firing downstream signaling and promoting lung tumorigenesis. [Abstract]2021 May 11;7(1):33. PMID: 33976114 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Cancer Lett
The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model. [Abstract]2017 Aug 1:400:61-68. PMID: 28455243
Alectinib Hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]
Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells are treated with 10 mM alectinib for various time points as indicated. The anti-b-Actin antibody is used as a loading control for whole cell extracts.
Alectinib Hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Aug 1:400:61-68. [Abstract]
In contrast to tumors treated with DMSO, tumors treated with Alectinib exhibits significantly decreased levels of p-Akt and p-S6. Furthermore, increased PARP and Caspase 3 cleavages are observed in tumors treated with Alectinib compared to controls.
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Cell Death Discov
The p53 activator overcomes resistance to ALK inhibitors by regulating p53-target selectivity in ALK-driven neuroblastomas. [Abstract]2018 May 10:4:56. PMID: 29760954
Alectinib Hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2018 May 10:4:56. [Abstract]
NB39-nu cells are treated with either 1000 nM Crizotinib (CR) or Alectinib (AL) for the indicated times and subjected to immunoblot analysis. CLTC is the loading control.
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Oncogene
ALK fusion promotes metabolic reprogramming of cancer cells by transcriptionally upregulating PFKFB3. [Abstract]2022 Sep;41(40):4547-4559. PMID: 36064579 -
Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
Aging Cell
2020 May;19(5):e13137. PMID: 32291952 -
Sci Signal
Host protein kinases required for SARS-CoV-2 nucleocapsid phosphorylation and viral replication. [Abstract]2022 Oct 25;15(757):eabm0808. PMID: 36282911 -
Pharmaceutics
Evaluation of Alectinib Metabolic Stability in HLMs Using Fast LC-MS/MS Method: In Silico ADME Profile, P450 Metabolic Lability, and Toxic Alerts Screening. [Abstract]2023 Oct 11;15(10):2449. PMID: 37896209 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Biomolecules
Lysophosphatidic Acid Stimulates Mitogenic Activity and Signaling in Human Neuroblastoma Cells through a Crosstalk with Anaplastic Lymphoma Kinase. [Abstract]2024 May 28;14(6):631. PMID: 38927035 -
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BMC Chem
Integrating analytical quality by design into bioanalytical method development: an HPLC-FLD method for quantification of alectinib in biological matrix. [Abstract]2025 Aug 22;19(1):248. PMID: 40847406 -
Cancer Sci
APE1 Attenuates ALK Tyrosine Kinase Inhibitors Sensitivity in NPM1-ALK Positive Anaplastic Large Cell Lymphoma. [Abstract]2025 Jul 23. PMID: 40702700 -
Transl Oncol
Anti-epidermal growth factor vaccine antibodies increase the antitumor activity of kinase inhibitors in ALK and RET rearranged lung cancer cells. [Abstract]2021 Jan;14(1):100887. PMID: 33129112 -
Neoplasia
ALK inhibitors downregulate the expression of death receptor 4 in ALK-mutant lung cancer cells via facilitating Fra-1 and c-Jun degradation and subsequent AP-1 suppression. [Abstract]2023 Aug:42:100908. PMID: 37192591 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
PLoS One
Inhibition of the anti-apoptotic protein BCL2 in EML4-ALK cell models as a second proposed therapeutic target for non-small cell lung cancer. [Abstract]2025 Jan 21;20(1):e0308747. PMID: 39836700 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Cell Physiol Biochem
Inhibition of Erythrocyte Cell Membrane Scrambling Following Energy Depletion and Hyperosmotic Shock by Alectinib. [Abstract]2018;51(5):1996-2009. PMID: 30522123 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Biol Pharm Bull
Evaluation of Drug-Induced Kidney Injury by Primary Culture of Rat Kidney Tissue Slices Using Oxygen-Permeable Polyolefin Plate with Low Drug Adsorption. [Abstract]2026;49(1):122-129. PMID: 41565252 -
Biomed Chromatogr
Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]2024 Oct;38(10):e5986. PMID: 39136165 -
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Heliyon
Quality by design-based approach for the development of an analytical method for quantifying ponatinib in rat plasma. [Abstract]2024 Sep 28;10(19):e38637. PMID: 39403541 -
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bioRxiv
The FDA-approved drug Alectinib compromises SARS-CoV-2 nucleocapsid phosphorylation and inhibits viral infection in vitro. [Abstract]2020 Dec 16:2020.08.14.251207. PMID: 32817937
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 2 mg/mL (3.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690. [Content Brief]
[2]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9265 mL | 9.6324 mL | 19.2649 mL | 48.1621 mL |
Alectinib Hydrochloride Related Classifications
HY-13011A Related Classifications
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