Alectinib

• 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[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

• Product Name Alternative:

  CH5424802; RO5424802; RG7853

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• 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.html

• Purity:

  99.94

• Solubility:

  DMSO : 4.33 mg/mL (ultrasonic)

• Smiles:

  N#CC1=CC2=C (C3=C (N2) C (C) (C4=CC (N5CCC (CC5) N6CCOCC6) =C (C=C4C3=O) CC) C) C=C1

• Molecular Formula:

  C30H34N4O2

• Molecular Weight:

  482.62

• Precautions:

  H302, H315, H319, H335

• 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:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Citation 01:

  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.|Biomolecules. 2024 May 28;14 (6) :631.|Cancer Res. 2022 Feb 1;82 (3) :484-496.|Microchem J. 2025 Nov 3;219:116046.

• CAS Number:

  1256580-46-7