Alectinib

• Product Name Alternative:

  CH5424802; RO5424802; RG7853

• UNSPSC 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].

• Target Antigen:

  Anaplastic lymphoma kinase (ALK)

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Field of Research:

  Cancer

• Assay Protocol:

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

• Purity:

  99.59

• 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 Weight:

  482.62

• 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.Aging Cell. 2020 May;19(5):e13137.|Biomed Chromatogr. 2024 Oct;38(10):e5986.|bioRxiv. 2020 Dec 16:2020.08.14.251207.|bioRxiv. November 12, 2021.|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.|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 Jan 10;100911.|Cell Rep Med. 2024 Mar 19;5(3):101472.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Exp Cell Res. 2020 Aug 1;393(1):112054.|Fundam Clin Pharmacol. 2021 Feb 1.|Harvard Medical School LINCS LIBRARY|Heliyon. 2024 Sep 28;10(19):e38637.|Mol Syst Biol. 2023 Dec 18.|Nat Cancer. 2022 Jun 20.|Nat Commun. 2022 Oct 3;13(1):5745.|Neoplasia. 2023 May 14;42:100908.|Oncogene. 2022 Sep 5.|Oncogene. 2022 Sep;41(40):4547-4559.|Pharmaceutics. 2023 Oct 11, 15(10), 2449.|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.|Cancer Res. 2022 Feb 1;82(3):484-496.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

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

• Clinical Information:

  Launched

• CAS Number:

  1256580-46-7