Ulixertinib

• Description :

  Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of [1][2].

• Product Name Alternative :

  BVD-523; VRT752271

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  ERK

• Type :

  Reference compound

• Related Pathways :

  MAPK/ERK Pathway; Stem Cell/Wnt

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/VRT752271.html

• Purity :

  99.95

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  O=C(C1=CC(C2=CC(NC(C)C)=NC=C2Cl)=CN1)N[C@@H](C3=CC=CC(Cl)=C3)CO

• Molecular Formula :

  C21H22Cl2N4O2

• Molecular Weight :

  433.33

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Ward RA, et al. Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem. 2015 Jun 11;58 (11) :4790-801.|[2]Kumar R, et al. Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. J Pharm Biomed Anal. 2016 Jun 5;125:140-4.|[3]Changwen Ning, et al. Targeting ERK Enhances the Cytotoxic Effect of the Novel PI3K and mTOR Dual Inhibitor VS-5584 in Preclinical Models of Pancreatic Cancer. Oncotarget. 2017 Jul 4;8 (27) :44295-44311.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

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

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  ERK1; ERK2

• Citation 01 :

  ACS Comb Sci. 2019 Dec 9;21 (12) :805-816.|Adv Sci (Weinh) . 2022 Oct;9 (30) :e2200717.|Adv Sci (Weinh) . 2024 Nov 20:e2407662.|Biomed Chromatogr. 2020 Oct;34 (10) :e4923.|bioRxiv. 2025 Mar 28:2025.03.25.645097.|Cancer Biol Ther. 2022 Dec 31;23 (1) :69-82.|Cancer Lett. 2024 Nov 26:217339.|Cancer. 2020 Mar 15;126 (6) :1339-1350.|Cancers (Basel) . 2022 Feb 14;14 (4) :954.|Cancers (Basel) . 2022 Mar 19;14 (6) :1575.|Cell Death Differ. 2024 Jun;31 (6) :804-819.|Cell Death Discov. 2022 Aug 17;8 (1) :365.|Cell Rep Med. 2025 Feb 6:101970.|Cell Rep. 2021 Dec 28;37 (13) :110174.|Dev Cell. 2020 Sep 14;54 (5) :608-623.e5.|Front Cell Dev Biol. 2018 Sep 25:6:111.|Innate Immun. 2020 Aug;26 (6) :505-513.|J Gastroenterol. 2024 Apr 29.|J Invest Dermatol. 2021 Apr;141 (4) :852-862.e6.|J Transl Med. 2025 Feb 28;23 (1) :244.|Life Sci. 2025 May 15:369:123553.|Matrix Biol. 2022 Sep:112:20-38.|Mol Cell Endocrinol. 2024 Mar 1:582:112140.|Nat Commun. 2022 Jul 14;13 (1) :4078.|Nat Commun. 2023 May 19;14 (1) :2859.|Nat Commun. 2023 Nov 2;14 (1) :6997.|Neoplasia. 2024 Dec 4:59:101085.|Pharmacol Res. 2023 Nov:197:106955.|Platelets. 2024 Dec;35 (1) :2354833.|Ren Fail. 2025 Dec;47 (1) :2580064.|Research Square Preprint. 2024 Nov 26.|Research Square Print. 2023 Feb 22.|Sci Adv. 2023 Nov 15;9 (46) :eadi5921.|Sci Data. 2024 Sep 19;11 (1) :1024.|Sci Rep. 2025 Jul 1;15 (1) :21328.|Sci Transl Med. 2021 Jan 27;13 (578) :eaba7308.|Theranostics. 2022 Oct 3;12 (16) :7051-7066.|Ulm University. Molecular Medicine Ulm. 2021 Mar.|Cancer Res. 2024 Jun 14;84 (12) :1963-1977.

• CAS Number :

  [869886-67-9]