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Alectinib (Hydrochloride)

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 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[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

Product Specifications

CAS Number

[1256589-74-8]

Product Name Alternative

CH5424802 (Hydrochloride) ; RO5424802 (Hydrochloride) ; AF-802 (Hydrochloride)

UNSPSC

12352005

Hazard Statement

H341, H361, H373

Target

Anaplastic lymphoma kinase (ALK)

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CH5424802-Hydrochloride.html

Purity

99.92

Solubility

DMSO : 2 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C30H35ClN4O2

Molecular Weight

519.08

Precautions

H341, H361, H373

References & Citations

[1]Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19 (5), 679-690.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Citation 01

Biomolecules. 2024 May 28;14 (6) :631.|Cancer Res. 2022 Feb 1;82 (3) :484-496.|Microchem J. 2025 Nov 3;219:116046.|Aging Cell. 2020 May;19 (5) :e13137.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biomed Chromatogr. 2024 Oct;38 (10) :e5986.|bioRxiv. 2020 Dec 16:2020.08.14.251207.|bioRxiv. November 12, 2021.|BMC Chem. 2025 Aug 22;19 (1) :248.|Cancer Discov. 2016 Oct;6 (10) :1118-1133. |Cancer Discov. 2018 Jun;8 (6) :714-729.|Cancer Discov. 2024 Sep 13:OF1-OF20.|Cancer Lett. 2017 Aug 1:400:61-68.|Cancer Sci. 2025 Jul 23.|Cell Death Discov. 2018 May 10:4:56.|Cell Discov. 2021 May 11;7 (1) :33.|Cell Physiol Biochem. 2018;51 (5) :1996-2009. |Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Cell Rep Med. 2024 Mar 19;5 (3) :101472.|Cell. 2025 Mar 6;188 (5) :1248-1264.e23.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Fundam Clin Pharmacol. 2021 Oct;35 (5) :919-929.|Harvard Medical School LINCS LIBRARY|Heliyon. 2024 Sep 28;10 (19) :e38637.|Leukemia. 2025 Aug 14.|Mol Syst Biol. 2024 Jan;20 (1) :28-55.|Nat Cancer. 2022 Jun;3 (6) :710-722.|Nat Commun. 2022 Oct 3;13 (1) :5745.|Neoplasia. 2023 Aug:42:100908.|Oncogene. 2022 Sep;41 (40) :4547-4559.|Patent. US20250003968A1.|Pharmaceutics. 2023 Oct 11;15 (10) :2449.|PLoS One. 2025 Jan 21;20 (1) :e0308747.|Research Square Preprint. 2024 Nov 26.|Sci Signal. 2022 Oct 25;15 (757) :eabm0808.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Science. 2014 Oct 3;346 (6205) :1255784.|Science. 2017 Dec 1;358 (6367) :eaan4368.|Transl Oncol. 2021 Jan;14 (1) :100887.|University of California. 2024.

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